- Total synthesis of inubosin B
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Inubosin B is the most active member of the acridine alkaloids isolated from Streptomyces sp. IFM 11440 culture. The inubosins initiate neuroregeneration via a neurogenine 2 pathway. In this work, we have described the total synthesis of inubosin B via two synthetic routes. The effects of various coupling, cyclization and reduction reactions are discussed including common pitfalls and side reactions. Reverse phase chromatography with TFA was crucial for the isolation of the product from aluminum ions present in the reduction media.
- Hamissa, Mohamed Farouk,Niederhafner, Petr,?afa?ík, Martin,Telus, Marta,Kolá?ová, Lenka,Koutná, Leah,?estáková, Hana,Sou?ek, Radko,?ebestík, Jaroslav
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Read Online
- AZAINDOLE DERIVATIVE AND USE THEREOF AS FGFR AND C-MET INHIBITOR
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A series of pyrazolopymidine derivatives, and use thereof in the preparation of a medicament for treating disease associated with FGFR and c-Met. The pyrazolopymidine derivative is a compound represented by formula (I), a tautomer, or a pharmaceutically acceptable salt thereof.
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Paragraph 0107
(2021/05/29)
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- NEW CLASS OF DNA GYRASE AND/OR TOPOISOMERASE IV INHIBITORS WITH ACTIVITY AGAINST GRAM-POSITIVE AND GRAM-NEGATIVE BACTERIA
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The present invention relates to compounds having a structure of general formula (I), processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment of bacterial infections in humans and warm-blooded animals.
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- SPIROCYCLIC INDOLONE POLYETHYLENE GLYCOL CARBONATE COMPOUND, COMPOSITION, PREPARATION METHOD AND USE THEREOF
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The present invention relates to a spirocyclic indolone polyethylene glycol carbonate compound, a composition thereof, a preparation method therefor, and a use thereof as an anticancer drug due to the antitumor activity thereof. The structural formula of the spirocyclic indolone polyethylene glycol carbonate compound is shown below. The compound has excellent tumor inhibitory activity, water solubility, low toxicity, and can be used for intravenous injection.
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- Spiroindolone polyethylene glycol carbonate compound, and compositions, preparation method and application thereof
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The invention relates to a spiroindolone polyethylene glycol carbonate compound, compositions and a preparation method thereof, and an application of the spiroindolone polyethylene glycol carbonate compound as an anticancer drug due to antitumor activity of the spiroindolone polyethylene glycol carbonate compound. The spiroindolone polyethylene glycol carbonate compound has a structural formula asdescribed in the specification, has excellent tumor suppressive activity, good water solubility and low toxicity, and can be used for intravenous injections.
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- Acylhydrazone compounds with anti-tumor activity as well as preparation method and application of acylhydrazone compounds
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The invention belongs to the technical field of medicinal chemistry, and in particular relates to acylhydrazone compounds with anti-tumor activity as well as a preparation method and application of the acylhydrazone compounds. The structures of the acylhydrazone compounds are as shown in a general formula (I) shown in the description, wherein R and R' are independently selected from any one or more of halogen, amino, cyano, alkoxy, 3,4-methylenedioxy, nitro, phenyl or substituted phenyl, and R and R' substituents are mono-substituted, disubstituted or tri-substituted. The preparation method issimple; biological activity test results of the compounds show that the compounds have a very good inhibitory effect on histone methyltransferase SET7, and have good application prospect in the development of anti-tumor aspects.
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Paragraph 0031; 0032; 0033; 0034
(2018/05/16)
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- Synthesis of the γ-Secretase Modulator MK-8428
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The synthesis of the γ-secretase modulator MK-8428 (1) is described. The synthesis is highlighted by an enzyme-catalyzed reaction to access 3,4,5-trifluoro-(S)-phenylglycine, a 1-pot activation/displacement/deprotection sequence to introduce the aminooxy functionality and a dehydrative intramolecular cyclization under mild conditions to form the oxadiazine heterocycle of 1. In situ reaction monitoring was employed to understand the deleterious role of water during the formation of a methanesulfonate ester in the 1-pot activation/displacement/deprotection sequence.
- Miller, Steven P.,Morris, William J.,Orr, Robert K.,Eckert, Jeffrey,Milan, Jay,Maust, Mathew,Cowden, Cameron,Cui, Jian
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p. 2957 - 2964
(2017/03/23)
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- CYSTOBACTAMIDES
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The present invention provides cystobactamides of formula (I) and the use thereof for the treatment or prophylaxis of bacterial infections:
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- Synthesis and biological evaluation of cystobactamid 507: A bacterial topoisomerase inhibitor from Cystobacter sp.
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Abstract The first total synthesis of cystobactamid 507, a member of a class of new natural products with strong inhibitory activity towards bacterial topoisomerases, is reported. Synthetic key challenges are the central tetrasubstitued arene and the low chemical reactivity of anilines and ortho-phenolic and isopropoxy-substituted benzoic acids. Biological evaluations demonstrate that cystobactamid 507 inhibits several Gram-positive pathogens but at significantly lower concentrations than described for the larger members of this natural product family.
- Moreno, María,Elgaher, Walid A.M.,Herrmann, Jennifer,Schl?ger, Nadin,Hamed, Mostafa M.,Baumann, Sascha,Müller, Rolf,Hartmann, Rolf W.,Kirschning, Andreas
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p. 1175 - 1178
(2015/06/02)
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- BENZAMIDE DERIVATIVE
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The present invention relates to benzamide derivatives represented by formula (I) or pharmaceutically acceptable salts thereof.
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Paragraph 1539; 1540
(2015/03/16)
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- COMPOUNDS USEFUL FOR THE TREATMENT OF METABOLIC DISORDERS AND SYNTHESIS OF THE SAME
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The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.
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Page/Page column 79
(2014/10/18)
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- NOVEL COMPOUNDS FOR MODULATION OF ROR-GAMMA ACTIVITY
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The present invention relates to aryl sulfones and related compounds that are modulators of ROR-gamma receptors. The invention also provides pharmaceutical compositions comprising these modulators, and methods of modulating ROR-gamma receptors using them. Also provided are methods of using aryl sulfones and related compounds as modulators of ROR-gamma to treat ROR-gamma mediated diseases
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Paragraph 00729
(2014/03/22)
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- Discovery of biphenylacetamide-derived inhibitors of BACE1 using de novo structure-based molecular design
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β-Secretase (BACE1), the enzyme responsible for the first and rate-limiting step in the production of amyloid-β peptides, is an attractive target for the treatment of Alzheimer's disease. In this study, we report the application of the de novo fragment-based molecular design program SPROUT to the discovery of a series of nonpeptide BACE1 inhibitors based upon a biphenylacetamide scaffold. The binding affinity of molecules based upon this designed molecular scaffold was increased from an initial BACE1 IC50 of 323 μM to 27 μM following the synthesis of a library of optimized ligands whose structures were refined using the recently developed SPROUT-HitOpt software. Although a number of inhibitors were found to exhibit cellular toxicity, one compound in the series was found to have useful BACE1 inhibitory activity in a cellular assay with minimal cellular toxicity. This work demonstrates the power of an in silico fragment-based molecular design approach in the discovery of novel BACE1 inhibitors.
- Mok, N. Yi,Chadwick, James,Kellett, Katherine A. B.,Casas-Arce, Eva,Hooper, Nigel M.,Johnson, A. Peter,Fishwick, Colin W. G.
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supporting information
p. 1843 - 1852
(2013/05/08)
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- PYRAZOLO[1,5a]PYRIMIDINE DERIVATIVES AS IRAK4 MODULATORS
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Compounds of the formula I or II: wherein X, m, Ar, R1 and R2 are as defined herein. The subject compounds are useful for treatment of IRAK-mediated conditions.
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Page/Page column 60
(2012/02/01)
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- GAMMA SECRETASE MODULATORS
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In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
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Page/Page column 360
(2010/06/15)
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- Synthesis, structure-affinity relationships, and radiolabeling of selective high-affinity 5-HT4 receptor ligands as prospective imaging probes for positron emission tomography
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In a search for high-affinity receptor ligands that might serve for development as radioligands for the imaging of brain 5-HT4 receptors in vivo with positron emission tomography (PET), structural modifications were made to the high-affinity 5-HT4 antagonist (1-butylpiperidin-4-yl) methyl 8-amino-7-iodo-2,3-dihydrobenzo[b][1,4]dioxine-5-carboxylate (1, SB 207710). These modifications were made mainly on the aryl side of the ester bond to permit possible rapid labeling of the carboxylic acid component with a positron emitter, either carbon-11 (t1/2 = 20.4 min) or fluorine-18 (t1/2 = 109.7 min), and included (i) replacement of the iodine atom with a small substituent such as nitrile, methyl, or fluoro, (ii) methylation of the 8-amino group, (iii) opening of the dioxan ring, and (iv) alteration of the length of the N-alkyl goup. High-affinity ligands were discovered for recombinant human 5-HT4 receptors with amenability to labeling with a positron emitter and potential for development as imaging probes. The ring-opened radioligand, (([methoxy-11C]1-butylpiperidin-4-yl)methyl 4-amino-3-methoxybenzoate; [11C]13), showed an especially favorable array of properties for future evaluation as a PET radioligand for brain 5-HT4 receptors. This article not subject to U.S. Copyright. Published 2010 by the American Chemical Society.
- Xu, Rong,Hong, Jinsoo,Morse, Cheryl L.,Pike, Victor W.
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experimental part
p. 7035 - 7047
(2010/12/25)
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- GAMMA SECRETASE MODULATORS
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In its many embodiments, the present invention provides a novel class of heterocyclic compounds of Group A or Group, as defined herein, as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions
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Page/Page column 139
(2010/06/15)
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- SUBSTITUTED BENZOAZOLE PDE4 INHIBITORS FOR TREATING PULMONARY AND CARDIOVASCULAR DISORDERS
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The invention relates to substituted benzothiazoles, benzoxazoles—and their counterparts having pyridine and pyrimidine rings replacing the benzene ring—that are PDE4 inhibitors useful for treating stroke, myocardial infarct, and cardiovascular inflammatory conditions, to pharmaceutical compositions comprising these compounds, and to methods for the treatment of stroke, myocardial infarct, and cardiovascular inflammatory conditions in a mammal. The compounds have general formula I: in which A and B are carbocycles or heterocycles. A particular embodiment is
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Page/Page column 31; 32
(2009/05/28)
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- UREA TYPE CINNAMIDE DERIVATIVE
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Disclosed is a compound represented by the formula (I) below or a pharmacologically acceptable salt thereof. Also disclosed is a use of the compound or salt as a pharmaceutical product. (In the formula, Ar1 represents an imidazolyl group which may be substituted with a C1-6 alkyl group; Ar2 represents a phenyl group which may be substituted with a C1-6 alkoxy group; X1 represents a single bond; R1 and R2 respectively represent a C1-6 alkyl group or the like which may be substituted with a substituent such as a 5- to 14-membered aromatic heterocyclic group; and R3 represents a hydrogen atom or the like.)
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Page/Page column 48
(2009/02/10)
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- A scalable synthesis of MN-447, an antagonist for integrins αvβ3 and αIIbβ 3
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(2S)-Benzeneslfonylamino-3-[3-methoxy-4-{4-(1,4,5,6-tetrahydropyrimidin-2- ylamino)piperidin-1-yl}benzoylamino]propionic acid, MN-447, is a potent antagonist of the integrins αvβ33 and αIIbβ3 Herein, we report a novel synthetic protocol that produces MN-447 in an overall yield of 45%. This protocol, when compared with the original synthetic route for MN-447, is more cost-effective, requires fewer steps, does not require chromatographic purification of intermediates and MN-447, and increases the overall yield by 35%. This report focuses on the synthetic strategies that were developed for this protocol. Now, the large quantities of MN-447 that are needed for preclinical and toxicological studies can be readily obtained.
- Ishikawa, Minoru,Tsushima, Masaki,Kubota, Dai,Yanagisawa, Yumiko,Hiraiwa, Yukiko,Kojima, Yasuo,Ajito, Keiichi,Anzai, Naomichi
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p. 596 - 602
(2013/01/03)
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- Transition metals in organic synthesis, Part 85.1 A general approach to 1,6-dioxygenated carbazole alkaloids - first total synthesis of clausine G, clausine I, and clausine Z
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Using the palladium-catalyzed construction of the carbazole framework, a highly efficient route to 1,6-dioxygenated carbazole alkaloids has been developed and applied to the total synthesis of clausenine, 6- methoxymurrayanine, clausenol, clausine G, clausine I, and clausine Z. The three latter natural products have been synthesized for the first time. Thieme Stuttgart.
- B?rger, Carsten,Kn?lker, Hans-Joachim
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body text
p. 1698 - 1702
(2009/05/07)
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- PLATELET ADP RECEPTOR INHIBITORS
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Compounds are provided which are useful as platelet ADP receptor inhibitors, for treating thrombosis and for reducing the likelihood and/or severity of a secondary ischemic event in a patient.
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Page/Page column 54
(2008/06/13)
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- PROCESS FOR PRODUCTION OF CINNAMAMIDE DERIVATIVE
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A compound (8) represented by the formula: (8) wherein R1 represents a 6- to 14-membered aromatic hydrocarbon ring group which may have a substituent; and n represents 0 to 2, can be produced with good efficiency by reacting a compound (3) represented by the formula: (3) wherein R1 and n are as defined above; and Q represents a single bond or -CH(Y)- where Y represents a hydrogen atom or a C1-6 alkyl group] with 3-methoxy-4-(4-methyl-1H-imidazol-1-yl)benzaldehyde in the presence of a base.
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Page/Page column 50
(2008/12/07)
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- SALTS OF CYNNAMIDE COMPOUND OR SOLVATES THEREOF
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The invention provides crystals of dihydrochloride monohydrate of the compound of the following formula having an Aβ production inhibiting effect which crystals are characterized by exhibiting a diffraction peak at an angle of diffraction (2θ ± 0.2°) of 10.9° in powder X-ray diffractometry. Further, the invention also provides the compound in the form of various salts, crystal forms and amorphous forms which are suitable for the development of drugs.
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Page/Page column 14
(2008/12/07)
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- Synthesis of carbazoles and dibenzofurans via cross-coupling of o-iodoanilines and o-iodophenols with silylaryl triflates and subsequent Pd-catalyzed cyclization
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An efficient route to a variety of carbazoles and dibenzofurans has been developed. It involves the reaction of o-iodoanilines or o-iodophenols with silylaryl triflates in the presence of CsF to afford the N- or O-arylated products, which are subsequently cyclized using a Pd catalyst to carbazoles and dibenzofurans in good to excellent yields. By using this methodology, the carbazole alkaloid, mukonine has been synthesized in 76% overall yield in three steps.
- Liu, Zhijian,Larock, Richard C.
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p. 347 - 355
(2007/10/03)
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- Next-generation spirobenzazepines: Identification of RWJ-676070 as a balanced vasopressin V1a/V2 receptor antagonist for human clinical studies
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We have continued to explore spirobenzazepines as vasopressin receptor antagonists to follow up on RWJ-339489 (2), which had advanced into preclinical development. Further structural modifications were pursued to find a suitable backup compound for human clinical studies. Thus, we identified carboxylic acid derivative 3 (RWJ-676070; JNJ-17158063) as a potent, balanced vasopressin V1a/V2 receptor antagonist with favorable properties for clinical development. Compound 3 is currently undergoing human clinical investigation.
- Xiang, Min Amy,Rybczynski, Philip J.,Patel, Mona,Chen, Robert H.,McComsey, David F.,Zhang, Han-Cheng,Gunnet, Joseph W.,Look, Richard,Wang, Yuanping,Minor, Lisa K.,Zhong, H. Marlon,Villani, Frank J.,Demarest, Keith T.,Damiano, Bruce P.,Maryanoff, Bruce E.
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p. 6623 - 6628
(2008/03/18)
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- Morpholine type cinnamide compound
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The present invention relates to a compound represented by the formula (I): or a pharmacologically acceptable salt thereof, wherein R1, R2, R3, and R4 are the same or different and each represent a hydrogen atom or a C1-6 alkyl group; X1 represents a C1-6 alkylene group that may be substituted; Xa represents a methoxy group or a fluorine atom; Xb represents an oxygen atom or a methylene group, provided that Xb is only an oxygen atom when Xa is a methoxy group; and Ar1 represents an aryl group, pyridinyl group, aryloxy group, or pyridinyloxy group that may have a substituent such as a halogen atom; and to use of the compound or salt as a pharmaceutical agent.
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Page/Page column 32
(2008/06/13)
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- Multi-cyclic cinnamide derivatives
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The present invention provides a compound represented by the formula (I): or a pharmacologically acceptable salt thereof, wherein Ar1 represents an imidazolyl group that may be substituted with a C1-6 alkyl group, or the like, Ar2 represents a phenyl group that may be substituted with a C1-6 alkoxy group, or the like, X1 represents a double bond or the like, and Het represents an imidazolyl group that may be substituted with a C1-6 alkyl group, or the like, which is effective as a therapeutic or prophylactic agent for a disease caused by Aβ.
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Page/Page column 62
(2010/11/28)
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- Cinnamide compound
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The present invention relates to a compound represented by Formula (I): (wherein Ar1 represents an imidazolyl group which may be substituted with 1 to 3 substituents; Ar2 represents a pyridinyl group, a pyrimidinyl group, or a phenyl group which may be substituted with 1 to 3 substituents; X1 represents (1) —C≡C— or (2) a double bond etc. which may be substituted; R1 and R2 represent, for example, a C1-6 alkyl group or C3-8 cycloalkyl group which may be substituted) or a pharmacologically acceptable salt thereof and to the use thereof as pharmaceutical agents. The object of the present invention is to find a therapeutic or preventive agent for diseases caused by Aβ. According to the present invention, a therapeutic or preventive agents for diseases caused by Aβ can be provided.
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- THERAPEUTIC AGENT FOR RESPIRATORY DISEASE CONTAINING 4-HYDROXYPIPERIDINE DERIVATIVE AS ACTIVE INGREDIENT
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An agent for preventing/treating respiratory diseases contains, as an active ingredient, a compound represented by following Formula (I): wherein A is a group represented by L-W [wherein L is a bond or CH2; and W is O, SOn (wherein n is 0 to 2), or -NR7-(wherein R7 is hydrogen or lower alkyl)]; each of G1 and G2 is (CH2)r (wherein r is 0 to 2), provided that when n is 1, G1 and G2 may be bridged by lower alkylene; Y is a lower alkylene or (substituted) benzylidene; Z is a bond or O, provided that when Z is a bond, Y may form a 5- or 6-membered ring with carbon on the benzene ring; R1 is, for example, NO2, a lower alkoxycarbonyl, (substituted) carbamoyl, (protected) hydroxyl group, (protected) carboxyl, or (protected) N-hydroxycarbamoyl; each of R2and R3 is hydrogen, halogen, (halogenated) lower alkyl, (halogenated) lower alkoxy or NO2; each of R4 and R5 is, for example, hydrogen, halogen, (halogenated) lower alkyl, (halogenated) lower alkoxy, CN, or lower alkylsulfonyl; and R6 is hydrogen or lower alkyl, a salt thereof or a solvate of them. It has excellent antitussive activity when used as an agent for preventing/treating respiratory diseases such as lung cancer, common cold syndrome, pulmonary tuberculosis, pneumonia, acute bronchitis or chronic bronchitis.
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Page/Page column 31
(2008/06/13)
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- 2,4-DIOXO-3-QUINAZOLINYLARYL SULFONYLUREAS
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2,4-Dioxo-3-quinazolinylaryl sulfonylurea compounds are provided that are useful for the inhibition of ADP-platelet aggregation, particularly in the treatment of thrombosis and thrombosis related conditions or disorders.
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Page/Page column 52
(2008/06/13)
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- Process for the preparation of nonpeptide substituted spirobenzoazepine derivatives
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Novel spirobenzoazepine compounds, novel processes for the preparation of nonpeptide substituted spirobenzoazepine derivatives, and novel processes for the preparation of intermediates in the preparation of such derivatives. Novel intermediates in the preparation of nonpeptide substituted spirobenzoazepine derivatives.
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- Substituted spirobenzazepines
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The invention is directed to nonpeptide substituted benzazepines of Formula I, which are useful as vasopressin receptor antagonists for treating conditions associated with vasopressin receptor activity such as those involving increased vascular resistance and cardiac insufficiency, including congestive heart failure, hyponatremia, and hypertension, among others disclosed. Pharmaceutical compositions comprising a compound of Formula I and methods of treating conditions such as hypertension, congestive heart failure, cardiac insufficiency, coronary vasospasm, cardiac ischemia, liver cirrhosis, hyponatremia, renal vasospasm, renal failure, diabetic nephropathy, cerebral edema, cerebral ischemia, stroke, thrombosis, or water retention are also disclosed.
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- COMPOUNDS USEFUL AS AICARFT INHIBITORS
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Compounds of the formula:(where R1, R2 and R3 are defined in the specification) are inhibitors of AICARFT. These compounds, as well as their pharmaceutically acceptable salts, solvents, prodrugs, and pharmaceutically active metabolites, are useful in pharmaceutical compositions for treating diseases such as cancer.
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- Transition metal complexes in organic synthesis. Part 68: Iron-mediated total synthesis of mukonine and mukonidine by oxidative cyclization with air as the oxidizing agent
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The oxidative cyclization of 5-(2-amino-5-methoxycarbonylphenyl)-substituted tricarbonyl[η4-cyclohexa-1,3-diene]iron complexes by air in protic medium provides the corresponding tricarbonyl[η4-4a,9a-dihydro-9H-carbazole]iron complexes. This procedure is applied to the total synthesis of the 3-methoxycarbonylcarbazole alkaloids mukonine and mukonidine.
- Kn?lker, Hans-Joachim,Wolpert, Marcus
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p. 5317 - 5322
(2007/10/03)
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- Towards New Iron(III) Chelators: Synthesis and Complexing Ability of a Water-Soluble Tripodal Ligand Based on 2,2′-Dihydroxybiphenyl Subunits
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A new water-soluble iron(III) sequestering agent has been designed. The tris-bidentate tripodal ligand consists of three 2,2′-dihydroxybiphenyl subunits connected via amide linkages at their meta (4-) positions to a framework of the "tren" type. The key step of the synthesis involves the coupling of suitably substituted monophenyl moieties in order to obtain the biphenyl precursor. The deprotonation constants of the ligand, and the formation and deprotonation constants of the FeIII complex have been determined from potentiometric and spectrophotometric measurements. The results are compared with those of a previously described homologous ligand in which the chelating subunits are attached to the tren framework via the ortho (3-) position of the biphenyl rather than the 4-position.
- Baret, Paul,Beaujolais, Virginie,Beguin, Claude,Gaude, Didier,Pierre, Jean-Louis,Serratrice, Guy
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p. 613 - 619
(2007/10/03)
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- Benzimidazole derivatives
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Disclosed are compounds represented by the following chemical formula (I) and pharmacologically acceptable salts thereof which are novel compounds useful as anticancer agents, antiviral agents or antimicrobial agents. STR1
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- Efficient reagents for the synthesis of 5-, 7-, and 5,7-substituted indoles starting from aromatic amines: Scope and limitations
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Upon reaction with IPy2BF4, 4-substituted anilines give regioselectively the corresponding o-iodoanilines in nearly quantitative yield, in a process that can be carried out on a multigram scale. Palladium-catalyzed coupling of the resulting 2-iodoanilines with (trimethylsilyl)acetylene (TMSA), followed by efficient CuI-mediated nitrogen cyclization onto alkynes with concurrent elimination of the TMS substituent, allows a straightforward elaboration of 5-mono- and 5,7-disubstituted indoles from aromatic amines. This new approach to the aforementioned indoles does not requires protective groups on nitrogen at any step and can be adapted for preparing related 7-monosubstituted indoles. Moreover, examples iterating the process are given, allowing bis-annulation and sequential double annulation and resulting in synthesis of benzodipyrroles. Additionally, suitable conditions for iodination of some of the target indoles with IPy2BF4 are discussed.
- Ezquerra, Jesus,Pedregal, Concepcion,Lamas, Carlos,Barluenga, Jose,Perez, Marta,Garcia-Martin, Miguel Angel,Gonzalez, Jose M.
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p. 5804 - 5812
(2007/10/03)
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- The Synthesis of Stypandrol, a Toxic Binaphthalenetetrol Isolated from Stypandra imbiricata: New Syntheses of Dianellidin and Stypandrone
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New syntheses of the naphthalenoid natural products dianellidin (2) and stypandrone (20), which rely on the Fries rearrangement, are described.This methodology is then applied to the synthesis of stypandrol (1), a toxic naphthalenetetrol isolated from Stypandra imbiricata R.Br. ('blind grass').
- Rizzacasa, Mark A.,Sargent, Melvyn V.
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p. 1087 - 1097
(2007/10/02)
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