15939-85-2

Upstream product

• 94-56-4 2-aminophenylthioacetic acid 
• 68-11-1 mercaptoacetic acid 
• 615-36-1 2-bromoaniline 
• 6320-02-1 o-bromothiophenol 
• 96-32-2 bromoacetic acid methyl ester 
• 105-36-2 ethyl bromoacetate 
• 340130-94-1 ethyl 2-((2-bromophenyl)thio)acetate 
• 1389489-20-6 tert-butyl 2-((2-bromophenyl)thio)acetate 
• 147227-31-4 (2-bromophenyl)-pyrrolidin-1-yl-diazene 

Downstream Products

• 6320-02-1 o-bromothiophenol 
• 298-12-4 Glyoxilic acid 
• 904297-88-7 benzoic acid N'-[2-(2-bromo-phenylsulfanyl)-acetyl]-N'-isopropyl-hydrazide 
• 340130-94-1 ethyl 2-((2-bromophenyl)thio)acetate 
• 98434-47-0 2,4-dibromophenyl-thioacetic acid 

Relevant academic research and scientific papers

MALIC ENZYME INHIBITORS

The present invention relates to novel compounds useful as malic enzyme (ME) inhibitors, processes for their preparation and use of these compounds for the therapeutic treatment of disorders mediated by ME such as cancers (e.g. pancreatic ductal adenocarcinoma (PDAC)) in humans.

Synthesis of N-Glycosyl-2-oxindoles by Pd-Catalyzed N-Arylation of 1-Amidosugars

An efficient intramolecular Pd-catalyzed N-arylation of o-iodo-amidosugars for the synthesis of N-glycosylated oxindoles has been reported. The coupling reaction takes place in toluene and involves Pd(OAc)2/RuPhos catalytic systems in the presence of K2CO3. This versatile approach was extended successfully to the synthesis of other N-glycosylated heterocycles.

Diacylglycerol acyltransferase inhibitors

Provided herein are compounds of the formula (1): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.

NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS

Disclosed herein are compounds of formula Ar1-X-W-Ar2 wherein Ar1 and Ar2 represent aryl groups characterized generally as aromatic heterocycles (e.g. imidazolyl or tetrazolyl) or carbocycles (e.g. phenyl or naphthalenyl); the aryl groups are optionally substituted or fused with other heterocycles or carbocycles; the aryl groups can bear substituents such as alkyl, halo or O-alkyl. X is a heteroatom, a valence bond or an optionally substituted divalent methylene, and W represents a spacer; typical spacers include divalent alkylene or alkylene-amido, -amido or -oxy radicals, which may optionally be substituted (e.g. hydroxyl or oxo). A typical compound is a derivative of 2-(N-napthalenyltetrazolylthio)- N-(2-nitrophenyl)acetamide. The compounds have inhibitory activity against Wild Type and single or double mutant strains of HIV.

KINETICS AND MECHANISM OF OXIDATION OF (ARYLTHIO)ACETIC ACIDS BY PYRIDINIUM HYDROBROMIDE PERBROMIDE

Oxidation of several monosubstituted (phenylthio)acetic acids (PTAA) by pyridinium hydrobromide perbromide (PHPB) was studied in aqueous acetic acid.The reaction is first order with respect to PHPB.Michaelis-Menten type kinetics are observed with respect to (arylthio)acetic acid.The effect of solvent composition indicates that the transition state is more polar than the reactants.The formation constants of the intermediate substrate-PHPB complexes and the rates of their decomposition were determined at different temperatures.The rates of oxidation of para and meta-substituted (phenylthio)acetic acids were correlated with Hammett's substituent constants.The ρ value is -1.60 at 35 deg c.The rates of oxidation of ortho substituted compounds are correlated with Charton's triparametric equation.A mechanism involving the decomposition of the intermediate complex in the slow rate-determining step affording a sulphonium ion which hydrolyses in a subsequent fast step to the sulphoxide is proposed.