3381-73-5

Usage

Uses

α-Bromo-?4-?chlorophenylacetic acid is a useful reactant or reagent in organic synthesis.

InChI:InChI=1/C8H6BrClO2/c9-7(8(11)12)5-1-3-6(10)4-2-5/h1-4,7H,(H,11,12)

Upstream product

• 1878-66-6 4-chlorophenylacetic Acid 
• 6212-33-5 2-(4-Chlorophenyl)glycine 
• 33512-03-7 3-(4-chlorophenyl)oxirane-2,2-dicarbonitrile 

Downstream Products

• 4718-68-7 α--4-chlor-phenylessigsaeure 
• 133192-67-3 2-chloro-benzaldehyde [5-(4-chloro-phenyl)-4-oxo-thiazolidin-2-ylidene]-hydrazone 
• 92426-95-4 2-(2-chloro-anilino)-5-(4-chloro-phenyl)-thiazol-4-one 
• 92873-46-6 2-benzylamino-5-(4-chloro-phenyl)-thiazol-4-one 
• 24091-92-7 methyl 2-bromo-2-(4-chlorophenyl)acetate 
• 184879-14-9 methyl 2-(4-chlorophenyl)-2-(4-isopropylphenoxy)acetate 
• 80362-98-7 2-(4-Chlorophenyl)-5,6,7,8-tetrahydro-3-hydroxythiazolo[3,2-a]-pyridinium bromide 
• 655223-09-9 2-(2-propynyloxy)-2-(4-chlorophenyl)-acetic acid 
• 930779-79-6 (2S)-1-oxo-1-(pyrrolidin-1-yl)propan-2-yl 2-bromo-2-(4-chlorophenyl)acetate 
• 2387-23-7 1,3-Dicyclohexylurea 
• 73842-44-1 2-(4-chlorophenyl)-N-phenylglycine 
• 1446308-39-9 (R)-quinuclidin-3-yl 2-(4-chlorophenyl)-2-(piperidin-1-yl)acetate 
• 1446308-40-2 (3R)-3-(2-(4-chlorophenyl)-2-(piperidin-1-yl)acetoxy)-1-(2-oxo-2-phenylethyl)-1-azoniabicyclo[2.2.2]octane bromide 
• 939756-54-4 2-(4-chlorophenyl)-2-(piperidin-1-yl)acetic acid 

Relevant academic research and scientific papers

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.

Catalytic Asymmetric Conjugate Addition and Sulfenylation of Diarylthiazolidin-2,4-diones

This work reports the first application of diarylthiazolidin-2,4-diones as nucleophiles in asymmetric catalysis. By utilizing chiral amino acid-based (thio)urea-tertiary amines as the catalysts, we successively established asymmetric conjugate addition to nitroolefins and sulfenylation to N-(sulfanyl)-succinimides of diarylthiazolidin-2,4-diones. Two series of biologically important 5-aryl-5-substituted thiazolidin-2,4-diones were obtained with high enantio- and diastereoselectivities (up to >99% ee and >19:1 dr). The enantioenriched adducts were found to show satisfactory anticancer activities against three different cancer cell lines using the MTT assay. All of these successes depended on the development of a general and expedient synthetic strategy to provide diverse 5H-thiazolidin-2,4-diones.

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.

Process for the stereoselective preparation of (-)-halofenate and derivatives thereof

The present invention provides a compounds the formula (IV): and methods for producing an α-(phenoxy)phenylacetic acid compound of the formula: wherein R1 is a member selected from the group consisting of: each R2 is a member indepen

NOVEL CYLOPENTA[B]BENZOFURAN DERIVATIVES AND THE UTILIZATION THEREOF

The invention relates to novel cyclopenta[b]benzofuran derivatives, to a method for the production thereof and to their utilization for the production of medicaments, especially for the prophylaxis and/or therapy of acute or chronic diseases which are cha

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.

SYNTHESES D'ESTERS OU D'ACIDES α-HALOGENES A PARTIR DES GEM DICYANO EPOXIDES.

α-halogeno esters or α-halogenoacids were easily prepared by selective one pot reaction of gem-dicyano epoxides with halohydric acids in an alcoholic or aqueous media.