cas 154229-19-3, Abiraterone | Articles data

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Synthesis and biological evaluation of analogs of didehydroepiandrosterone as potential new anticancer agents
The synthesis, cytotoxicity and inhibition of CDK8 by thirteen analogs of cortistatin A are reported. These efforts revealed that the analogs with either a 6- or 7-isoquinoline or 5-indole side chain in the 17-position are the most promising anti-proliferative agents. These compounds showed potent cytotoxic effects in CEM, HeLa and HMEC-1 cells. All three compounds exhibited IC50 values 10μM. The most interesting 10l analog exhibited an IC50 value of 0.59 μM towards the human dermal microvascular endothelial cell line (HMEC-1), significantly lower than the reference standard 2-methoxyestradiol. At a concentration at 50 nM the most potent 10h compound reduced the activity of CDK8 to 35percent.
Hansen, Trond Vidar,Liekens, Sandra,Solu, Eirik J.
(2020)
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PRODRUGS OF ABIRATERONE
The present invention relates to compounds of formula (I), or their isotopic forms, stereoisomers, tautomers, or pharmaceutically acceptable salt(s) thereof as prodrugs of abiraterone. The present invention also describes method of making such compounds, pharmaceutical compositions comprising such compounds and the use of the compounds of formula (I).
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Page/Page column 21-22

(2021/05/29)

A new method for the synthesis of abiraterone drug catalyzed by Pd-NPs@Zn-MOF as efficient reusable catalyst
The present work provides a novel process for the preparation of abiraterone drug in a Suzuki–Miyaura coupling approach by a new heterogeneous palladium catalyst, Pd-NPs@Zn-MOF, which has been synthesized by one-step encapsulation in nanoporous metal–organic framework Zn-MOF under a temperature control program for the first time. Pd-NPs@Zn-MOF were characterized by transmission electron microscopy (TEM), X-Ray powder diffraction (XRD), BET surface area analysis, inductively coupled plasma (ICP)-optical emission spectrometry (OES), and X-ray photoelectron spectroscopy (XPS).
Mirjafary, Zohreh,Mokhtari, Javad,Shirazi, Seyed Mohammad Hossein
(2021/10/12)

Preparation method of abiraterone
The invention provides a preparation method of abiraterone, and belongs to the technical field of medicine synthesis. The preparation method comprises the following steps: by taking a compound 17-bromoandrostane-5, 16-diene-3beta-alcohol as an initial raw material, carrying out borylation reaction on the initial raw material and boric acid ester under the action of an accelerant to obtain an intermediate compound 2; and allowing the compound 2 and a pyridyl compound to be subjected to a coupling reaction under the action of a catalyst to obtain the abiraterone. According to the method, the yield and the purity of abiraterone are remarkably improved by adjusting the synthesis route, the ratio of the reaction raw materials and other process parameters; the preparation method disclosed by the invention is simple and easy to implement and mild in condition, the yield of the obtained product is as high as 95%, the purity of the product is as high as 99.8%, and the stipulation of the drug quality standard is met.
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Paragraph 0047; 0049-0051; 0053-0055; 0057-0067

(2022/01/04)

Slow-, tight-binding inhibition of CYP17A1 by abiraterone redefines its kinetic selectivity and dosing regimen
Substantial evidence underscores the clinical efficacy of inhibiting CYP17A1-mediated androgen biosynthesis by abiraterone for treatment of prostate oncology. Previous structural analysis and in vitro assays revealed inconsistencies surrounding the nature and potency of CYP17A1 inhibition by abiraterone. Here, we establish that abiraterone is a slow-, tight-binding inhibitor of CYP17A1, with initial weak binding preceding the subsequent slow isomerization to a high-affinity CYP17A1-abiraterone complex. The in vitro inhibition constant of the final high-affinity CYP17A1-abiraterone complex ( ( Ki? = 0.39 nM )yielded a binding free energy of -12.8 kcal/mol that was quantitatively consistent with the in silico prediction of 214.5 kcal/mol. Prolonged suppression of dehydroepiandrosterone (DHEA) concentrations observed in VCaP cells after abiraterone washout corroborated its protracted CYP17A1 engagement. Molecular dynamics simulations illuminated potential structural determinants underlying the rapid reversible binding characterizing the two-step induced-fit model. Given the extended residence time (42 hours) of abiraterone within the CYP17A1 active site, in silico simulations demonstrated sustained target engagement even whenmost abiraterone has been eliminated systemically. Subsequent pharmacokineticpharmacodynamic (PK-PD) modeling linking time-dependent CYP17A1 occupancy to in vitro steroidogenic dynamics predicted comparable suppression of downstream DHEA-sulfate at both 1000- and 500-mg doses of abiraterone acetate. This enabled mechanistic rationalization of a clinically reported PK-PD disconnect, inwhich equipotent reduction of downstreamplasma DHEAsulfate levels was achieved despite a lower systemic exposure of abiraterone. Our novel findings provide the impetus for reevaluating the current dosing paradigmof abiraterone with the aim of preserving PD efficacy while mitigating its dose-dependent adverse effects and financial burden. SIGNIFICANCE STATEMENT With the advent of novel molecularly targeted anticancer modalities, it is becoming increasingly evident that optimal dose selection must necessarily be predicated on mechanistic characterization of the relationships between target exposure, drug-target interactions, and pharmacodynamic endpoints. Nevertheless, efficacy has always been perceived as being exclusively synonymous with affinity-based measurements of drug-target binding. This work demonstrates how elucidating the slow-, tight-binding inhibition of CYP17A1 by abiraterone via in vitro and in silico analyses was pivotal in establishing the role of kinetic selectivity in mediating time-dependent CYP17A1 engagement and eventually downstream efficacy outcomes.
Cheong, Eleanor Jing Yi,Nair, Pramod C.,Neo, Rebecca Wan Yi,Tu, Ho Thanh,Lin, Fu,Chiong, Edmund,Esuvaranathan, Kesavan,Fan, Hao,Szmulewitz, Russell Z.,Peer, Cody J.,Figg, William D.,Chai, Christina Li Lin,Miners, John O.,Chan, Eric Chun Yong
supporting information
p. 438 - 451
(2020/09/04)

Synthetic method of abiraterone acetate and intermediate thereof (by machine translation)
The invention relates to a synthesis method of abiraterone acetate and a dragon intermediate thereof. In the synthesis method of abiraterone acetate intermediate, a compound of formula (I), a chloro reagent and a base are chlorinated to obtain the abiraterone acetate intermediate of formula (II). The mass ratio of the compound of the formula (I) to the base is 1: (1.5 -3). The structure of the compound of formula (I) and abiraterone acetate is as follows. To the synthesis method, the occurrence probability of side reactions in the chlorination reaction process can be reduced while the high reaction activity is maintained, so that the yield and purity of the abiraterone acetate intermediate can be improved, and the process is simple. (by machine translation)
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(2021/01/04)

Method for preparing abiraterone acetate
The invention provides a method for preparing abiraterone acetate. Specifically, the invention relates to an improved method for synthesizing abiraterone or a derivative thereof through a key 3 beta-benzoyloxy intermediate. According to the process, intermediate DHEA 3-benzoyloxy ester is a solid, the intermediate with higher purity can be obtained through a crystallization method, and the processoperability is high. Meanwhile, benzoyl is strong in electric negative force, easy to react with hydroxyl and high in acylation rate, and a six-membered ring structure is twisted in a space structureof a benzoyl functional group, so that elimination reaction is not easy to perform, and generation of process byproducts is effectively avoided.
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(2020/07/14)

Preparation method of abiraterone acetate
The invention provides a preparation method of abiraterone acetate: dissolving an alkenyl iodide (17-iodoandrostane-5,16-diene-3[beta]-acetate or 17-iodoandrostane-5,16-diene-3[beta]-hydroxyl), a compound (I), an aryl boride (diethyl(3-pyridyl)borane), a compound (II), pyridine-3-boronic acid or pyridine-3-boronic acid pinacol ester, an alkaline substance, and a Pd/C catalyst in an organic solvent, and performing a reaction at 60-120 DEG C for 3-12 h; after the reaction is finished, carrying out post-treatment on the reaction liquid to obtain the abiraterone acetate and recycling the Pd catalyst; wherein the compound (I) and compound (II) are represented as the formulas as follows. The method is high in yield, is less in impurity and has convenience of recycling the noble metal catalyst and obtaining raw materials, is simple in operation, is available to industrial production, and has great application value.
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Paragraph 0033-0035

(2019/05/15)

Structure-Based Design of Inhibitors with Improved Selectivity for Steroidogenic Cytochrome P450 17A1 over Cytochrome P450 21A2
Inhibition of androgen biosynthesis is clinically effective for treating androgen-responsive prostate cancer. Abiraterone is a clinical first-in-class inhibitor of cytochrome P450 17A1 (CYP17A1) required for androgen biosynthesis. However, abiraterone also causes hypertension, hypokalemia, and edema, likely due in part to off-target inhibition of another steroidogenic cytochrome P450, CYP21A2. Abiraterone analogs were designed based on structural evidence that B-ring substituents may favorably interact with polar residues in binding CYP17A1 and sterically clash with residues in the CYP21A2 active site. The best analogs increased selectivity of CYP17A1 inhibition up to 84-fold compared with 6.6-fold for abiraterone. Cocrystallization with CYP17A1 validated the intended new contacts with CYP17A1 active site residues. Docking these analogs into CYP21A2 identified steric clashes that likely underlie decreased binding and CYP21A2 inhibition. Overall, these analogs may offer a clinical advantage in the form of reduced side effects.
Fehl, Charlie,Vogt, Caleb D.,Yadav, Rahul,Li, Kelin,Scott, Emily E.,Aubé, Jeffrey
p. 4946 - 4960
(2018/06/20)

STEROIDAL COMPOUND, COMPOSITION CONTAINING THE SAME AND USE THEREOF
Provided in the present invention are a steroidal compound, a composition containing the same and a use thereof. Specifically, disclosed in the present invention are a steroidal compound as shown in formula (I) and a drug composition containing the same, or a crystal form, a pharmaceutically acceptable salt, a hydrate or solvate, a stereoisomer, a prodrug, a metabolite or an isotopic variant thereof. The compound according to the present invention can be used as a CYP17 enzyme inhibitor, and has better pharmacokinetic parameters, which can improve drug concentration of the compound in an animal, thereby improving the efficacy and safety of the drug, and in turn the compound may be applied in the preparation of the drug for treating CYP17 enzyme-related diseases (such as prostate cancer).
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Paragraph 0081

(2018/11/21)

Novel method for preparing abiraterone acetate
The invention relates to the technical field of medicines, and in particular relates to a novel method for preparing abiraterone acetate. The abiraterone acetate prepared according to the preparationmethod provided by the present application has a high yield and is easy to purify compared with the prior art, the method can reduce hydroxyl by-products and double- bond by-products generated duringthe reaction, a content of a single impurity is less than 0.1%, the preparation method is simple, the costs are suitable, raw materials have small toxicity, and the method is suitable for industrialized mass production.
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Paragraph 0078; 0085; 0086; 0087; 0088; 0089; 0090-0092

(2018/10/11)

A process for the production of acetate (by machine translation)
The invention belongs to the technical field of pharmaceutical and chemical industries, and in particular relates to a process for the production of acetate, this invention has improved the acetate synthetic route, to the dehydroepiandrosterone as raw materials, by condensation with hydrazine hydrate, iodo, with 3 - pyridine [...] coupled reactions, such as the acetylation 4 step reaction synthesizes the target product acetate, the overall yield is 51.4%. Is determined synthetic compound 17 - (3 - pyridyl) - androst - 5, 16 - diene - 3 β - ol the best reaction time and the reaction temperature is 5 h, 35 °C. The route mild reaction conditions, raw materials are cheap and easy to obtain, and the production cost is low. (by machine translation)
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Paragraph 0022; 0023; 0026; 0028; 0031; 0033

(2018/09/08)

Abiraterone acetate preparation method
The invention discloses an abiraterone acetate preparation method, and particularly provides an abiraterone acetate preparation process. In the prior art, the preparation process comprises a palladiumcatalyzed coupling reaction, the palladium catalyzed reaction can cause the pollution on the reaction product, and palladium is difficultly separated from the target product. According to the presentinvention, palladium is removed with the substituted phosphine-containing compound so as to effectively control the palladium residue.
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(2018/07/30)

Material used for abiraterone acetate refined products and synthetic method thereof
The invention belongs to the technical field of organic chemistry, and discloses a material used for abiraterone acetate refined products and a synthetic method thereof. The synthetic method of the material used for abiraterone acetate refined products is realized by reaction of acetate dehydroepiandrosterone, a compound B, a compound C, a compound D and a compound E. According to the invention, the synthetic route is short, reaction conditions are easily achieved, and compared with other synthetic routes, the material has the advantages that weak acid is adopted, corrosion to equipment is small, and single-step yields are all 85% or above.
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(2018/10/02)

Synthesis method of abiraterone acetate highly finished product
The invention belongs to the technical field of organic chemistry, and discloses a synthesis method of an abiraterone acetate highly finished product. The synthesis method comprises the following steps: sequentially adding absolute ethyl alcohol, hydrazine hydrate and glacial acetic acid in dehydroisoandrosterone 3-acetate (SM1), and preparing a reactant B at the temperature of 20-30 DEG C; addingtetrahydrofuran and iodine, slowly adding tetramethyl guanidine at the temperature of -5 to 5 DEG C, controlling the temperature to be 10 DEG C or below, and dropwise adding a tetrahydrofuran solution of the compound B at the temperature of -5 to 5 DEG C for 6 h to obtain a compound C; sequentially adding tetrahydrofuran, diethyl-(3-pyridine)borane, trans-dichlorobis(triphenyl-phosphine)palladiumand a tetrabutylammonium fluoride trihydrate in the compound C to obtain a compound D; and adding dichloromethane and 4-dimethylaminopyridine in the compound D, slowly adding acetic anhydride at thetemperature of 15-35 DEG C, and adding activated carbon and methanol-water after finishing the reaction to obtain a compound E, and highly finishing the compound E to prepare the abiraterone acetate highly finished product.
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(2018/12/02)

Synthesis of the anti-prostate cancer drug abiraterone acetate
Abiraterone acetate is used for the treatment of castration-resistant prostate cancer. Abiraterone acetate was synthesized from dehydroepiandrosterone via a three-step reaction including the formation of tosylhydrazone, cross-coupling reaction and acetylation, and a two-step purification including column chromatography and recrystallization with an overall yield of 51.9%. Here, an improved procedure for the preparation of abiraterone acetate is described. This synthetic process is of easy operation and low cost, which is suitable for industrialization.
Ma, Siyue,Li, Jianheng,Tang, Huayang,Xu, Feng
p. 461 - 469
(2018/03/27)

Steroid compound and preparation method thereof
The invention relates to a steroid compound impurity in production of abiraterone acetate. The steroid compound is 17-(ethyl)androsta-5,16-diene-3beta-ol acetate (as shown in a formula I which is described in the specification). A preparation method for the steroid compound comprises the following steps: reacting sulfonic acid ester of dehydroisoandrosterone acetate with diethyl(3-pyridyl)borane; then carrying out reduced-pressure distillation and separation so as to obtain an intermediate 17-(ethyl)androsta-5,16-diene-3beta-ol; and then carrying out acetylation so as to obtain the steroid compound. The steroid compound as shown in the formula I can be applied to qualitative and quantitative research on and detection of impurities in raw abiraterone acetate.
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Paragraph 0044; 0045; 0046; 0047

(2017/10/13)

A new method for synthesizing acetate (by machine translation)
The invention relates to a new method for synthesizing acetate, which belongs to the field of drug synthesis, more specifically, relates to the treatment of advanced prostate cancer drug acetate new synthetic method and in the synthetic method relates to new intermediates for the preparation of compounds. This invention adopts the acetic acid pregnancy double-alkene alcohol ketone as raw materials, by methyl R base asia sulphone lithium reagent addition and rearrangement reaction to obtain the catalyst product 3, the catalyst 3 by oxidation and hetero D - A, isomerization, acetylation reaction such as synthesis of the compound of acetate. The invention solves the problems of the prior art synthetic materials of the more expensive the cost problem, provides a high yield, environmental pollution is small, simple and of the purified preparation [...] acetate method, this method is comparatively easy to amplification to the industrial production. (by machine translation)
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Paragraph 0008; 0022;

(2017/09/29)

A acetate synthesis method
The invention relates to a synthesis method of abiraterone acetate. According to the synthesis method of the abiraterone acetate, a compound 1 is taken as a revelator, and the abiraterone acetate is prepared through steps such as esterification, Grignard reagent reaction, dehydration, acylation, reduction, acetylation and the like.
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Paragraph 0054; 0094; 0095; 0096

(2017/08/31)

A method for avoiding heavy metal residual acetate preparation method
The invention discloses a novel method for preparing abiraterone acetate. The method comprises the following steps of: hydroxyl protection, Aldol reaction, dehydration reaction, deprotection and acetylation. According to the method, the heavy-metal reagent, the strict anhydrous and anaerobic equipment and the expensive alkyl boron reagent are not used, thus the cost is reduced greatly. The method is suitable for mass industrial production.
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(2017/08/25)

Synthesis method of abiraterone acetate
The invention discloses a synthesis method of abiraterone acetate. The method includes: taking dehydroepiandrosterone as the raw material, conducting condensation with p-toluenesulfonhydrazide, then carrying out coupling reaction with 3-bromopyridine, and conducting acetylation so as to synthesize the target product abiraterone acetate. According to the synthesis method provided by the invention, the route has mild reaction conditions, the raw materials are cheap and easily available, and the production cost is low.
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Paragraph 0025; 0026; 0033; 0034; 0041; 0042

(2017/09/02)

A method for preparing arab League bit Long Yi ester (by machine translation)
The invention discloses a method for preparing arab League bit Long Yi acid ester, comprising the following steps: acetic acid dehydro epandrosterone and 3-chloropyridine Grignard reagent in diethyl ether as the solvent, generate condensation reaction, after dehydration prepared crude ester arab League bit Long Yi ; arab League bit Long Yi ester crude product in methanol as the solvent, hydrolysis under alkaline conditions, make 17 - (3-pyridyl)-androsta -4,16-diene -3 β-ol; 17 - (3-pyridyl)-androsta -4,16-diene -3 β- mellow heavy crystallization; 17 - (3-pyridyl)-androsta -4,16-diene -3 β-ol arab League bit Long Yi acid ester prepared by reaction with acetyl chloride. The method of the invention has the advantages of simple operation, the raw materials used are cheap and easily obtained, mild reaction conditions, low equipment requirements, high total yield, the used solvent synchronization recovery, and the like, the production cost is low, large-scale production is easy, has significant industrial application value. (by machine translation)
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Paragraph 0038; 0039; 0040

(2016/12/07)

ALTERING STEROID METABOLISM FOR TREATMENT OF STEROID-DEPENDENT DISEASE
A method of treating steroid-dependent disease such as prostate cancer in a subject is described that includes administering a therapeutically effective amount a CYP17A inhibitor and an effective amount of a 5- -reductase inhibitor to the subject.
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Page/Page column 47;48

(2016/09/26)

INHIBITORS OF CYP17A1
Compounds according to formula I or II are provided. Such compounds are useful in treating cancers, such as leukemia, colon cancer, breast cancer, or prostate cancer by beneficially inhibiting CYP17A1. Pharmaceutical compositions and methods including the compounds are also provided.
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Paragraph 0102

(2016/04/05)

A method for preparing abiraterone acetate (by machine translation)
The invention relates to a method for preparing abiraterone acetate, the method is to dehydrogenation epandrosterone as raw materials, with hydrazine hydrate, iodine response, to obtain 17-iodo-androst -5,16-diene -3 β-ol, then the under the catalysis of palladium benzene phosphine base43 with 3-pyridine zinc halide occurs arab League bit dragon Negishi coupling reaction, the final with acetyl chloride or acetic anhydride esterification, to obtain the target product abiraterone acetate. (by machine translation)
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(2017/02/09)

Abiraterone acetate and wherein the intermediate preparation method
The invention relates to a method for preparing abiraterone which is a key intermediate of abiraterone acetate serving as a medicament for treating prostatic cancer and a method for preparing the abiraterone acetate by using the intermediate thereof. The methods are simple in processes, and the products have high purity and low content of impurities.
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Paragraph 0097 - 0099

(2017/04/03)

Preparation method of abiraterone acetate
The invention provides a preparation method of abiraterone acetate. According to the method, firstly an intermediate product, namely coarse abiraterone is purified and refined, then a purified product of abiraterone is acetylated, the abiraterone acetate is directly prepared, accordingly the coarse abiraterone product which is in an off-white color, relatively high in purity and less in impurity is obtained directly, the coarse abiraterone product is further simply crystallized, the abiraterone acetate which is high in purity and meets the medicinal requirement can be obtained, and therefore the step of chromatography or tedious purification of an inorganic salt-precipitated crystal in a traditional method can be avoided. The method has the advantages of being more convenient and faster in operation and purification treatment step, more suitable for industrialized amplification production and the like.
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Paragraph 0012; 0087; 0089; 0090

(2016/10/09)

An improved method for synthesizing arab League bitlong Zhi acetic acid
The invention discloses an improved abiraterone acetate synthesis method. A known synthesis process is improved in the invention, a reaction solvent is changed, an appropriate temperature is selected and the catalyst dosage is reduced, so that the reaction conditions are more mild, the raw material cost is lower, the operation is simpler, the yield is higher, the product is easier to purify and a technical support is provided for industrial production of abiraterone acetate.
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Paragraph 0036; 0037; 0039

(2016/10/08)

AN IMPROVED PROCESS FOR THE PREPARATION OF ABIRATERONE ACETATE
The present invention relates to an improved process for the preparation of abiraterone acetate. More specifically the invention relates to a process for the preparation of abiraterone acetate free from dimer and other impurities.
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(2015/07/16)

PROCESS FOR THE PREPARATION OF UNSATURATED TRIFLUOROMETHANESULFONATE STEROID DERIVATIVES
Disclosed is a method for the conversion of a compound of formula 3 to a compound of formula 4, wherein R is an acetyl group or an alcohol-protecting group. The process involves reacting 3 with a triflating agent in the presence of a nicotinate (3-pyridinecarboxylate) of a C1-C4 alcohol, preferably methyl nicotinate (methyl 3-pyridinecarboxylate) or ethyl nicotinate (ethyl 3-pyridinecarboxylate), to give 4. The method can be conveniently used in a process for the preparation of Abiraterone or Abiraterone acetate.
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(2015/12/05)

PROCEDURE FOR THE PREPARATION OF ABIRATERONE ACETATE AND INTERMEDIATES THEREOF
Disclosed is a process for the preparation of abiraterone and abiraterone acetate with high yields and purity. A key element of the method is the isolation of a crystalline intermediate that makes the process particularly suitable for implementation on an industrial scale.
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Paragraph 11; 12

(2015/09/23)

PROCESS FOR THE PREPARATION OF ABIRATERONE AND INTERMEDIATES THEREOF
The present invention provides intermediates for preparing abiraterone, and processes for preparing abiraterone and intermediates thereof. The intermediates include a compound of formula (IV): wherein R represents a hydroxy-protecting group.
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Paragraph 0146

(2015/02/05)

PROCESS FOR ABIRATERONE ACETATE
The present invention provides a novel process for the preparation of abiraterone. The present invention also provides a novel process for the preparation of abiraterone acetate.
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Page/Page column 6; 7

(2014/07/21)

SYNTHESIS OF ABIRATERONE AND RELATED COMPOUNDS
The present invention relates to processes for obtaining abiraterone and derivatives thereof, such as abiraterone acetate, by means of a Suzuki coupling through a steroid borate of general formula (IV) or a C—C coupling through a steroid hydrazone of general formula (II), as well as to intermediates useful in said processes.
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(2014/02/15)

PROCESS FOR THE PURIFICATION OF ABIRATERONE ACETATE
The invention relates to a process for the purification of crude abiraterone acetate by treatment with polymer resins in aqueous solvent. The purified product is recovered by simple concentration and filtration.
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Page/Page column 8

(2014/05/24)

PROCESS FOR THE PREPARATION OF (3β)-17-(3-PYRIDINYL)ANDROSTA-5,16-DIEN-3-YL ACETATE AND POLYMORPH THEREOF
The present invention relates to a process for the preparation of (3β)-17-(3- pyridinyl)androsta-5,16-dien-3-yl acetate compound of formula- 1. The present invention also relates to a novel polymorph of compound of formula- 1 and process for its preparation.
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Page/Page column 19; 20

(2014/12/12)

Improved procedure for preparation of abiraterone acetate
An improved procedure for the preparation of abiraterone acetate is described. The present process highlights reduced reaction time, isolation with acid-base treatment without involving column chromatography, multiple crystallization and is amenable to la
Madhra, Mukesh Kumar,Sriram, Hari Mohan,Inamdar, Murad,Sharma, Mukesh Kumar,Prasad, Mohan,Joseph, Sony
p. 555 - 558
(2014/05/06)

PROCESS AND INTERMEDIATES FOR THE PREPARATION OF ABIRATERONE ACETATE
The present invention relates to a process for the synthesis of (3beta)17-(3- pyridinyl)androsta-5,16-dien-3-yl acetate (Abiraterone acetate) represented by the structure of formula (1), and salts thereof, especially salts with pharmaceutically acceptable acids. The present invention further relates to certain intermediates in such processes.
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(2014/02/16)

SYNTHESIS OF ABIRATERONE AND RELATED COMPOUNDS
The present invention relates to processesfor obtaining abirateroneand derivatives thereof, such as abiraterone acetate, by means of a Suzuki coupling through a steroid borate of general formula (IV) or a C-C coupling through a steroid hydrazone of general formula (II), as well as to intermediates useful in said processes.
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(2013/03/28)

Processes for the preparation of abiraterone and related compouds
The present invention relates to processes for obtaining abiraterone and derivatives thereof, such as abiraterone acetate, by means of a C-C coupling through a steroid hydrazone of general formula (II) or a Suzuki coupling through a steroid borate of general formula (IV), as well as to intermediates useful in said processes.
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(2013/07/19)

PROCESS FOR PREPARING 17-SUBSTITUTED STEROIDS
The present invention relates to a process for the preparation of 17-substituted steroids and, more particularly, to an improved method of synthesizing abiraterone or derivatives thereof in high yield and purity by means of a key 3-formate intermediate.
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Page/Page column 12; 13; 15; 16; 18; 20; 21

(2013/04/25)

CYP11B, CYP17, AND/OR CYP21 INHIBITORS
Provided herein are inhibitors of CYP11B, CYP17, and/or CYP21 enzymes of Formula (Z), (IX), (X), (XI), (XII), (XIII), (XIV), (XV), (XVI), or (XVII). Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat androgen-dependent diseases, disorders and conditions. Formula (Z)
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Page/Page column 224

(2012/06/30)

SYNTHESIS OF 17-(3-PYRIDYL) STEROIDS
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(2008/06/13)

17-substituted steroids useful in cancer treatment
Compounds of the general formula (1) STR1 wherein X represents the residue of the A, B and C rings of a steroid, R represents a hydrogen atom or an alkyl group of 1 to 4 carbon atoms, R 14 represents a hydrogen atom and R 15 represents a hydrogen atom or an alkyl or alkoxy group of 1-4 carbon atoms, or a hydroxy or alkylcarbonyloxy group of 2 to 5 carbon atoms or R 14 and R 15 together represent a double bond, and R 16 represents a hydrogen atom or an alkyl group of 1 to 4 carbon atoms, in the form of the free bases or phannaceutically acceptable acid addition salts, are useful for treatment of androgen-dependent disorders, especially prostatic cancer, and also oestrogen-dependent disorders such as breast cancer.
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(2008/06/13)

A convenient, large-scale synthesis of abiraterone acetate [3β-acetoxy-17-(3-pyridyl)androsta-5,16-diene], a potential new drug for the treatment of prostate cancer
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Potter, Gerard A.,Hardcastle, Ian R.,Jarman, Michael
p. 123 - 128
(2007/10/03)

Novel Steroidal Inhibitors of Human Cytochrome P45017α (17α-Hydroxylase-C17,20-lyase): Potential Agents for the Treatment of Prostatic Cancer
Steroidal compounds having a 17-(3-pyridyl) substituent together with a 16,17-double bond have been synthesized, using a palladium-catalyzed cross-coupling reaction of a 17-enol triflate with diethyl(3-pyridyl)borane, which are potent inhibitors of human testicular 17α-hydroxylase-C17,20-lyase.The requirement for these structural features is stringent: compounds having 2-pyridyl (9), 4-pyridyl (10), or 2-pyridylmethyl (11) substituents instead of the 3-pyridyl substituent were either poor inhibitors or noninhibitory.Reduction of the 16,17-double bond to give 17β-pyridyl derivatives diminished potency with 3-pyridyl substitution (327; IC50 for lyase, 2.923 nM) but increased it with a 4-pyridyl substituent present (1028; IC50 1 μM53 nM).In contrast, a variety of substitution patterns in rings A-C of the steroid skeleton afforded inhibitors having potencies similar to those most closely related structurally to the natural substrates pregnenolone and progesterone, respectively 17-(3-pyridyl)androsta-5,16-dien-3β-ol (3, Kiapp 1 nM; IC50 for lyase, 2.9 nM) and 17-(3-pyridyl)androsta-4,16-dien-3-one (15; IC50 for lyase, 2.1 nM).Thus compounds having variously aromatic ring A (18), saturated rings A/B (21,22), and oxygenated ring C (26) exhibited IC50 values for lyase (1.8-3.0 nM) falling within a 2-fold range.The most potent compounds are candidates for development as drugs for the treatment of hormone-dependent prostatic carcinoma.
Potter, Gerard A.,Barrie, S. Elaine,Jarman, Michael,Rowlands, Martin G.
p. 2463 - 2471
(2007/10/02)

Chemical Properties

Appearance/Colour :white solid
Melting Point: 227-228 °C(Solv: toluene (108-88-3))
Boiling Point: 500.17 °C at 760 mmHg
Flash Point:256.294 °C
Density: 1.14 g/cm³
Solubility:Chloroform (Slightly), Methanol (Slightly)
Storage Temp.:2-8°C
Vapor Pressure: 7.99E-11mmHg at 25°C
Refractive Index: 1.605
PKA: 14.71±0.70(Predicted)
PSA: 33.12000
LogP: 5.39860

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Suzhou Lipin chemical Co., Ltd.
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Min Order:1 Gram
FOB Price:No Data
Main Products:32
Country:

Golden Pharma Co., Limited
Business Type:Other
Min Order:1 Kilogram
FOB Price:No Data
Main Products:47
Country:

Kono Chem Co.,Ltd
Business Type:Other
Min Order:1 Kilogram
FOB Price:No Data
Main Products:86
Country:

Wuhan Fortuna Chemical Co.,Ltd
Business Type:Trading Company
Min Order:100 Gram
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Main Products:51
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Henan Allgreen Chemical Co.,Ltd
Business Type:Manufacturers
Min Order:1 Gram
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Main Products:34
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Ality Chemical Corporation
Business Type:Other
Min Order:1
FOB Price:No Data
Main Products:165
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Xi'an Xszo Chem Co., Ltd.
Business Type:Manufacturers
Min Order:1 Gram
FOB Price:USD $ 0.1-0.1 / Gram
Main Products:108
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Shanghai Seasonsgreen Chemical Co.,Ltd
Business Type:Manufacturers
Min Order:1 Kilogram
FOB Price:USD $ 1.0-1.0 / Kilogram
Main Products:36
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Dayang Chem (Hangzhou) Co.,Ltd.
Business Type:Lab/Research institutions
Min Order:1 Kilogram
FOB Price:USD $ 2.0-2.0 / Kilogram
Main Products:994
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Hebei yanxi chemical co.,LTD.
Business Type:Trading Company
Min Order:1 Metric Ton
FOB Price:USD $ 1.0-3.0 / Metric Ton
Main Products:84
Country:

Chemwill Asia Co., Ltd.
Business Type:Manufacturers
Min Order:5 Kiloliter
FOB Price:USD $ 1.2-5.0 / Kiloliter
Main Products:56
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Hubei DiBo chemical co., LTD
Business Type:Other
Min Order:25 Kilogram
FOB Price:USD $ 1.0-2.0 / Kilogram
Main Products:34
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Henan Tianfu Chemical Co., Ltd.
Business Type:Lab/Research institutions
Min Order:1 Kilogram
FOB Price:No Data
Main Products:67
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Hebei Nengqian Chemical Import and Export Co., LTD
Business Type:Trading Company
Min Order:1 Kilogram
FOB Price:USD $ 1.0-10.0 / Kilogram
Main Products:162
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Zhuozhou Wenxi import and Export Co., Ltd
Business Type:Trading Company
Min Order:1 Kilogram
FOB Price:USD $ 139.0-210.0 / Kilogram
Main Products:1
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Henan Sinotech Import&Export Corporation
Business Type:Other
Min Order:1 Metric Ton
FOB Price:USD $ 1.0-1.0 / Metric Ton
Main Products:20
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LIDE PHARMACEUTICALS LIMITED
Business Type:Lab/Research institutions
Min Order:1 Gram
FOB Price:No Data
Main Products:56
Country:

Hebei Sankai Chemical Technology Co., Ltd
Business Type:Trading Company
Min Order:1 Kilogram
FOB Price:USD $ 60.0-65.0 / Kilogram
Main Products:11
Country:

Hangzhou Sartort Biopharma Co., Ltd
Business Type:Lab/Research institutions
Min Order:1 Kilogram
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Main Products:80
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Hubei Langyou International Trading Co., Ltd
Business Type:Other
Min Order:10 Gram
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Main Products:15
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Article Database

154229-19-3

Articles about 154229-19-3Total 46 be found

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Chemical Properties

Appearance/Colour :white solid

Melting Point: 227-228 °C(Solv: toluene (108-88-3))

Boiling Point: 500.17 °C at 760 mmHg

Flash Point:256.294 °C

Density: 1.14 g/cm³

Solubility:Chloroform (Slightly), Methanol (Slightly)

Storage Temp.:2-8°C

Vapor Pressure: 7.99E-11mmHg at 25°C

Refractive Index: 1.605

PKA: 14.71±0.70(Predicted)

PSA: 33.12000

LogP: 5.39860

Global suppliers and manufacturers of 154229-19-3total 202 suppliers on LookChem

Article Database

154229-19-3

Articles about 154229-19-3Total 46 be found

More Articles about upstream products of 154229-19-3

More Articles about downstream products of 154229-19-3

Chemical Properties

Appearance/Colour :white solid

Melting Point: 227-228 °C(Solv: toluene (108-88-3))

Boiling Point: 500.17 °C at 760 mmHg

Flash Point:256.294 °C

Density: 1.14 g/cm3

Solubility:Chloroform (Slightly), Methanol (Slightly)

Storage Temp.:2-8°C

Vapor Pressure: 7.99E-11mmHg at 25°C

Refractive Index: 1.605

PKA: 14.71±0.70(Predicted)

PSA: 33.12000

LogP: 5.39860

Global suppliers and manufacturers of 154229-19-3total 202 suppliers on LookChem

Density: 1.14 g/cm³