199679-74-8

Upstream product

• 851754-08-0 4S-benzyl-3-[3-(4-chlorophenyl)-2R-methylpropionyl]oxazolidin-2-one 
• 64-18-6 formic acid 
• 70090-69-6 1-chloro-4-(prop-2-yn-1-yl)benzene 
• 52085-96-8 3-(4-chlorophenyl)propanoyl chloride 
• 2019-34-3 3-(4-chlorophenyl)propanoic acid 
• 1202-60-4 -2-methyl-3-(4-chlorophenyl)prop-2-enoic acid 
• 117763-47-0 methyl 3-(4-chlorophenyl)-2-methylpropanoate 

Relevant academic research and scientific papers

Enantioselective Synthesis of Chiral Carboxylic Acids from Alkynes and Formic Acid by Nickel-Catalyzed Cascade Reactions: Facile Synthesis of Profens

We report a stereoselective conversion of terminal alkynes to α-chiral carboxylic acids using a nickel-catalyzed domino hydrocarboxylation-transfer hydrogenation reaction. A simple nickel/BenzP* catalyst displayed high activity in both steps of regioselective hydrocarboxylation of alkynes and subsequent asymmetric transfer hydrogenation. The reaction was successfully applied in enantioselective preparation of three nonsteroidal anti-inflammatory profens (>90 % ees) and the chiral fragment of AZD2716.

ISOXAZOLYL SUBSTITUTED BENZIMIDAZOLES

A compound which is a benzimidazolyl isoxazole of formula (I): wherein: R0and R, which are the same or different, are each H or C1-6 alkyl; R9, R9 and R9, which are the same or different, are each H o

Design, synthesis, in vitro, and in vivo characterization of phenylpiperazines and pyridinylpiperazines as potent and selective antagonists of the melanocortin-4 receptor

Benzylamine and pyridinemethylamine derivatives were synthesized and characterized as potent and selective antagonists of the melanocortin-4 receptor (MC4R). These compounds were also profiled in rodents for their pharmacokinetic properties. Two compounds with diversified profiles in chemical structure, pharmacological activities, and pharmacokinetics, 10 and 12b, showed efficacy in an established murine cachexia model. For example, 12b had a Ki value of 3.4 nM at MC4R, was more than 200-fold selective over MC3R, and had a good pharmacokinetic profile in mice, including high brain penetration. Moreover, 12b was able to stimulate food intake in the tumor-bearing mice and reverse their lean body mass loss. Our results provided further evidence that a potent and selective MC4R antagonist with appropriate pharmacokinetic properties might potentially be useful for the treatment of cancer cachexia.

Asymmetric hydrogenation of α,β-unsaturated carboxylic acids catalyzed by ruthenium(II) complexes of spirobifluorene diphosphine (SFDP) ligands

The ruthenium diacetate complexes ligated by chiral spirobifluorene diphosphines (SFDP) were very effective catalysts for the asymmetric hydrogenation of tiglic acid derivatives and α-methylcinnamic acid derivatives with high activities and excellent enantioselectivities (up to 98% ee). The α-aryloxybutenoic acids can also be hydrogenated by these catalysts to provide the corresponding saturated α-aryloxybutanoic acids in high yields (89-93%) and enantioselectivities (up to 95% ee). In this reaction, the SFDP ligand with para-methyl groups on the P-phenyl rings gave the best results.

Highly rigid diphosphane ligands with a large dihedral angle based on a chiral spirobifluorene backbone

High and wide: The high rigidity and large dihedral angle of chiral, spirobifluorene-based diphosphane ligands lead to excellent reactivity and enantioselectivity in the ruthenium-catalyzed asymmetric hydrogenation of α,β-unsaturated carboxylic acids (see scheme).

Enantioselective hydrolysis of some 2-aryloxyalkanoic acid methyl esters and isosteric analogues using a penicillin G acylase-based HPLC monolithic silica column

A technique based on liquid chromatography has been developed to facilitate studies of enantioselectivity in penicillin G acylase (PGA)-catalyzed hydrolysis of some 2-aryloxyalkanoic acid methyl esters and isosteric analogues. PGA was covalently immobilized on an aminopropyl monolithic silica support to create an immobilized HPLC-enzyme reactor. Two sets of experimental data were drawn to calculate the enantioselectivity (E) of the kinetically controlled enantiomer-differentiating reaction, the degree of substrate conversion and the enantiomeric excess of the product. The developed enzymatic reactor was coupled through a switching valve to an achiral analytical column for separation and quantitation of the hydrolysis products. The enantiomeric excess was determined off-line on a PGA-chiral stationary phase. In this way, highly precise E values were determined. A computational study related to the hydrolysis of the considered racemic esters was also carried out in order to unambiguously clarify both the substrate specificity and the enantioselectivity displayed by PGA.