cas 29270-30-2, 2-Bromo-2-(2'-chlorophenyl) acetic acid

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Method for preparing clopidogrel intermediate alpha-bromo (2-chloro) methyl phenylacetate by recycling aqueous solution method
The invention provides a method for preparing clopidogrel intermediate alpha-bromo (2-chloro) methyl phenylacetate by recycling an aqueous solution method. According to the method, o-chlorophenylacetic acid is adopted as a main raw material, an organic solvent and water in an appropriate proportion are optimized to serve as a bromination mixed solvent, a two-phase reaction mode is adopted in the reaction process, a bromine-containing wastewater solution can be reused without complex treatment, a target product is prepared through bromination and esterification reactions, and the yield reaches78% or above; the method provided by the invention is based on a technical scheme of recycling an aqueous solution containing a bromination reagent. In the process production process, the input amountof a new bromination reagent is reduced to a great extent, the bromine atom utilization rate of the bromination reagent is increased, the problems of wastewater treatment and discharge are reduced, the pressure of environmental pollution is reduced, meanwhile, the reaction conditions are relatively mild, treatment is simple, and industrial production is facilitated.
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Paragraph 0021-0028

(2020/08/22)

Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer
The bromodomain and extra-terminal proteins (BET) have emerged as promising therapeutic targets for the treatment of castration-resistant prostate cancer (CRPC). We report the design, synthesis and evaluation of a new series of benzoxazinone-containing 3,5-dimethylisoxazole derivatives as selective BET inhibitors. One of the new compounds, (R)-12 (Y02234), binds to BRD4(1) with a Kd value of 110 nM and blocks bromodomain and acetyl lysine interactions with an IC50 value of 100 nM. It also exhibits selectivity for BET over non-BET bromodomain proteins and demonstrates reasonable anti-proliferation and colony formation inhibition effect in prostate cancer cell lines such as 22Rv1 and C4-2B. The BRD4 inhibitor (R)-12 also significantly suppresses the expression of ERG, Myc and AR target gene PSA at the mRNA level in prostate cancer cells. Treatment with (R)-12 significantly suppresses the tumor growth of prostate cancer (TGI = 70%) in a 22Rv1-derived xenograft model. These data suggest that compound (R)-12 is a promising lead compound for the development of a new class of therapeutics for the treatment of CRPC.
Xue, Xiaoqian,Zhang, Yan,Wang, Chao,Zhang, Maofeng,Xiang, Qiuping,Wang, Junjian,Wang, Anhui,Li, Chenchang,Zhang, Cheng,Zou, Lingjiao,Wang, Rui,Wu, Shuang,Lu, Yongzhi,Chen, Hongwu,Ding, Ke,Li, Guohui,Xu, Yong
supporting information
p. 542 - 559
(2018/05/24)

Synthesis and Antibacterial Screening of 1,3,4-Thiadiazoles, 1,2,4-Triazoles, and 1,3,4-Oxadiazoles Containing Piperazine Nucleus
A series of novel 1,3,4-thiadiazoles, 1,2,4-triazoles, and 1,3,4-oxadiazoles were synthesized by cyclization of substituted 1-(2-(2-chlorophenyl)-2-(4-(2,3-dichlorophenyl)piperazin-1-yl)acetyl)thiosemicarbazide. The structures of all newly synthesized compounds were elucidated on the basis of spectral studies. Some of them were screened for their antibacterial activity. The compounds 6b, 6c, 8e, 9a, and 9b have shown moderate activity towards Bacillus Subtilis and Escherichia Coli.
Deshmukh, Rajendra,Karale, Bhausaheb,Akolkar, Hemantkumar,Randhavane, Pratibha
p. 1355 - 1360
(2017/03/27)

Clopidogre and wherein the intermediate α-bromo-ortho-chlorophenyl acetic acid and α-thiophene substituted ethylamino- method for the preparation of acetic acid hydrochloride (by machine translation)
The invention discloses a preparation method of clopidogrel and intermediates thereof. The preparation method of the clopidogrel and intermediates thereof, provided by the invention, has the characteristics of being simple to operate, mild in reaction condition, little in pollution, low in energy consumption and the like and is suitable for industrial production, a high-purity intermediate can be provided for production of the clopidogrel, and the production cost of the clopidogrel is reduced.
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Paragraph 0051-0053

(2017/04/29)

BENZOFUROPYRIMIDINONES AS PROTEIN KINASE INHIBITORS
A compound according to formula I: or a pharmaceutically acceptable salt thereof; wherein R1, R2, R3a, R3b, R3c and R3d are as defined in the specification, pharmaceutical compositions thereof, and methods of use thereof.
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Page/Page column 243

(2009/08/14)

N-PHENYL HYDRAZIDES AS MODULATORS OF THE GHRELIN RECEPTOR
The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein: each R1 is independently selected from the group consisting of Cl, Br, CH3 and CF3; X is carbon or nitrogen; R1a is H or a straight C1-3 alkyl group; R2a is H or a methyl group R2 is selected from the group consisting of C1-3alkyl, H and -(CH2)n-, wherein n is 3 or 4 and the terminal carbon of the chain is bonded to the carbon atom adjacent to the nitrogen bearing the R2 group, such that a fused 6,5 or 6,6-bicyclic ring is formed. Y is selected from the group consisting of: phenyl which may be unsubstituted or substituted by one or more substituents independently selected from the group consisting of C1-3alkyl, C1-3alkoxy, halogen, C1-3alkyl substituted by 1 to 7 fluoro atoms and C1-3alkoxy substituted by 1 to 7 fluoro atoms; pyridyl which may be unsubstituted or substituted by one or more substituents independently selected from the group consisting of C1-3alkyl, OCH3, CF3, CN, and halogen; naphthyl which may be unsubstituted or substituted by one or more substituents independently selected from the group consisting of F and OCH3; pyrimidinyl; imidazo[1,2-a]pyridine-6-yl; benzothiophen-2-yl; benzothiophen-5-yl; benzofuran-2-yl; dibenzo[b,d]furan-3-yl; dibenzo[b,d]thiophen-2-yl; dibenzo[b,d]thiophen-4-yl; 1,3- benzodioxol-5-yl; 2,3-dihydro-1,4-benzodioxin-5-yl; 2,3-dihydro-1,4-benzodioxin-6-yl; 2,3- dihydro-1-benzofuran-4-yl; 2,2-difluoro-1,3-benzodiox-4-yl; pyridazinyl; imidazolyl; oxazolyl; pyrazolyl; thiazolyl; and triazolyl; with the proviso that when Y is 2,3-dihydro-1,4-benzodioxin-6-yl, R1 is not Cl; processes for their preparation, intermediates useble in these processes, pharmaceutical compositions containing them and their use in therapy, for example as modulators of of the growth hormone secretagogue receptor (also referred to as the ghrelin receptor or GHSR1a receptor) and/or for the treatment and/or prophylaxis of a disorder mediated by the ghrelin receptor.
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Page/Page column 51

(2009/01/24)

Design and synthesis of non-cytotoxic tetrahydrothieno[3,2-c]pyridine derivatives exhibiting complement inhibition activity
A series of 4,5,6,7-tetrahydrothieno[3,2-c]pyridine derivatives have been synthesized and evaluated for their activity on the activation of human complement (classical pathway) and their intrinsic haemolytic activity. The in vitro assay results of these analogues for inhibition of complement activity reveals improved inhibitory activity for some of the analogues over existing tetrahydrothienopyridine derivatives like Ticlopidine and Clopidogrel. Significantly, these analogues did not exhibit any haemolytic activity and are non-cytotoxic to human cell lines.
Master, Hoshang E.,Khan, Shabana I.,Poojari, Krishna A.
p. 97 - 105
(2008/09/20)

THE METHOD OF MAKING OPTICALLY ACTIVE 2-HALO-2-(N-SUBSTITUTED PHENYL)ACETIC ACID ESTERS AND 2-HALO-2-(N-SUBSTITUTED PHENYL)ACETIC ACIDS BY ENZYMATIC METHOD
The present invention relates to the process for the preparation of optically active 2-halo-2-(n-substituted phenyl)acetic acid esters and optically active 2-halo-2-(n-substituted phenyl)acetic acids, which are used intensively as important chiral intermediates, represented by general formula 2 and 3 respectively from racemic 2-halo-2-(n-substituted phenyl)acetic acid ester represented by general formula 1. In more detail, this invention relates to the process for preparing optically active 2-halo-2-(n-substituted phenyl)acetic acid esters and optically active 2-halo-2-(n-substituted phenyl)acetic acids by stereospecific hydrolysis of racemic 2-halo-2-(n-substituted phenyl)acetic acid esters using hydrolases or hydrolase-producing microorganisms in the aqueous phase or organic phase including aqueous solvent. This method is useful in the practical process because the production and separation of compounds with high optical purity is easier.
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Page/Page column 4

(2008/06/13)

Anti-viral compounds
The present invention relates to compounds of Formula (I) below, which inhibit the growth of picornaviruses, Hepatitus viruses, enteroviruses, cardioviruses, polioviruses, coxsackieviruses of the A and B groups, echo virus and Mengo virus. wherein: A is phenyl, pyridyl, substituted phenyl, substituted pyridyl, or benzyl; R is hydrogen, COR4, or COCF3; X is N—OH, O, or CHR1; R1is hydrogen, halo, CN, C1-C4alkyl, —C≡CH, CO(C1-C4alkyl), CO2(C1-C4alkyl), or CONR2R3; R2and R3are independently hydrogen or C1-C4alkyl; A′ is hydrogen, halo, C1-C6alkyl, benzyl, naphthyl, thienyl, furyl, pyridyl, pyrollyl, COR4, S(O)nR4, or a group of the formula R4is C1-C6alkyl, phenyl, or substituted phenyl; n is 0, 1, or 2; R5is independently at each occurrence hydrogen or halo; m is 1, 2, 3, or 4; and R6is hydrogen, halo, CF3, OH, CO2H, NH2, NO2, CONHOCH3, C1-C4alkyl, or CO2(C1-C4alkyl), C1-C4alkoxy; or a pharmaceutically acceptable salt thereof.
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(2008/06/13)

Process for the preparation of α-bromo-phenylacetic acids
Compounds of formula STR1 in which R1 and R2 are hydrogen or halogen, are prepared by reacting an aldehyde of formula: STR2 with CHBr3 and KOH in a mixture of an inert solvent and water. Further an ester of compound (I) wherein R1 is H and R2 is 2-Cl is reacted with 4,5,6,7-tetrahydrothieno[3,2-c]pyridine to produce a compound of formula III: STR3 which is useful as a medicament.
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(2008/06/13)