71283-66-4

Upstream product

• 66648-29-1 methyl 2-{[(4-methylphenyl)sulfonyl]oxy}propanoate 
• 27871-49-4 (S)-Methyl lactate 
• 104-15-4 toluene-4-sulfonic acid 
• 98-59-9 p-toluenesulfonyl chloride 

Downstream Products

• 91-20-3 naphthalene 
• 119393-06-5 methyl (S)-2-(naphthalen-2-yl)propionate 
• 222722-14-7 methyl (R)-2-(naphthalen-2-yl)propionate 
• 22561-78-0 methyl (S)-2-(naphthalen-1-yl)propionate 
• 267668-18-8 methyl (R)-(+)-2-(phenylthio)propanoate 
• 89402-39-1 (R)(+)-2-[4-(3-fluoro-5-trifluoromethylpyridin-2-yloxy)-phenoxy]-propionic acid methyl ester 
• 57646-33-0 methyl (2R)-2-[(2,6-dimethylphenyl)amino]propanoate 
• 922178-61-8 ?(R)-3-methylpiperazin-2-one 
• 89402-41-5 (R)(+)-2[4-(5-chloro-3-fluoro-pyridin-2-yloxy)-phenoxy]-propionic acid-methyl ester 

Relevant academic research and scientific papers

Biobased High-Performance Aromatic-Aliphatic Polyesters with Complete Recyclability

The development of high-performance recyclable polymers represents a circular plastics economy to address the urgent issues of plastic sustainability. Herein, we design a series of biobased seven-membered-ring esters containing aromatic and aliphatic moie

Selective NK-3 receptor antagonist, preparation and application thereof

The invention provides a selective NK-3 receptor antagonist, preparation and application thereof, particularly a compound represented by the following formula (I). The compound of the invention has unexpected activity to modulate cytokines and/or interferon, and is useful in the treatment of CNS and peripheral diseases or disorders.

Unveiling the active isomer of cycloalanopine, a cyclic opine from: Lactobacillus rhamnosus LS8, through synthesis and analog production

Opines are widely distributed natural products formed by the reductive condensation of amino acids with α-keto acids or carbonyls of carbohydrates. They have important biological roles in bacteria, higher plants, fungi, invertebrates and mammals, including humans. An unusual cyclic opine of undefined stereochemistry, cycloalanopine, was previously isolated from Lactobacillus rhamnosus LS8 and reported to have antimicrobial activity against both Gram-negative and Gram-positive bacteria. In this work, we report a three-step strategy to synthetically access pure isomers of this cyclic compound and analogs thereof. In the key step, acyclic bis-hydrazides can be oxidized with (diacetoxyiodo) benzene to corresponding cyclic N,N-diacylhydrazides. The three cycloalanopine isomers, along with several analogs, were synthesized and tested against a panel of Gram-positive and Gram-negative bacteria. We identified the active isomer as the meso compound: (4R,6S)-4,6-dimethyl-1,2,5-triazepan-3,7-dione. Additionally, a glycine derivative, (R)-4-methyl-1,2,5-triazepan-3,7-dione, was ascertained to be more potent. This compound was active against both Gram-positive and Gram-negative organisms with the strongest potency against Escherichia coli and Acinetobacter baumannii, an opportunistic pathogen found in hospital-derived infections.

Optimization of Orally Bioavailable PI3KδInhibitors and Identification of Vps34 as a Key Selectivity Target

Optimization of a lead series of PI3Kδinhibitors based on a dihydroisobenzofuran core led to the identification of potent, orally bioavailable compound 19. Selectivity profiling of compound 19 showed similar potency for class III PI3K, Vps34, and PI3Kδ, and compound 19 was not well-tolerated in a 7-day rat toxicity study. Structure-based design led to an improvement in selectivity for PI3Kδover Vps34 and, a focus on oral phramacokinetics properties resulted in the discovery of compound 41, which showed improved toxicological outcomes at similar exposure levels to compound 19.

Synthesis method of optically active metalaxyl

The invention discloses a synthesis method of optically active metalaxyl. The optically active metalaxyl is synthesized by performing methoxylation and acylating chlorination on chloroacetic acid to obtain methoxyacetyl chloride and then reacting Methoxyacetyl chloride with D-N-(2,6-dimethylphenyl) alanine methyl ester; a one-pot method operation is adopted for the synthesis; the two-step reactionof methoxylation and acylating chlorination is directly used for a next-step reaction without post-treatment. According to the process of the optically active metalaxyl, by adopting the one-pot method operation, the operation steps are simplified, the production of three wastes is decreased, the synthesis cost is reduced, the obtained product is stable in quality and relatively high in output andyield, and the synthesis method is suitable for large-scale production.

Synthesis of dendrimer-type chiral stationary phases based on the selector of (1S,2R)-(+)-2-amino-1,2-diphenylethanol derivate and their enantioseparation evaluation by HPLC

In our recent work, a series of dendritic chiral stationary phases (CSPs) were synthesized, in which the chiral selector was L-2-(p-toluenesulfonamido)-3- phenylpropionyl chloride (selector I), and the CSP derived from three-generation dendrimer showed the best separation ability. To further investigate the influence of the structures of dendrimer and chiral selector on enantioseparation ability, in this work, another series CSPs (CSPs 1-4) were prepared by immobilizing (1S,2R)-1,2-diphenyl-2-(3-phenylureido)ethyl 4-isocyanatophenylcarbamate (selector II) on one- to four-generation dendrimers that were prepared in previous work. CSPs 1 and 4 demonstrated the equivalent enantioseparation ability. CSPs 2 and 3 showed the best and poorest enantioseparation ability respectively. Basically, these two series of CSPs exhibited the equivalent enantioseparation ability although the chiral selectors were different. Considering the enantioseparation ability of the CSP derived from aminated silica gel and selector II is much better than that of the one derived from aminated silica gel and selector I, it is believed that the dendrimer conformation essentially impacts enantioseparation.

PIPERIDINE-4-ACETIC ACID DERIVATIVES AND THEIR USE

The present invention is directed to compounds of formula (I) compositions comprising them and their use.

USE OF PIPERIDINE DERIVATIVES AS AGONISTS OF CHEMOKINE RECEPTOR ACTIVITY

The present invention is directed to novel piperidinc derivatives and to the use of piperidine derivatives of formula (I) as agonists of chemokine receptor activity.

Enantioselective synthesis of allenamides via sulfimide [2,3]-sigmatropic rearrangement

Chiral allenamides are prepared with high levels of enantiomeric purity by [2,3]-sigmatropic rearrangement of propargylic sulfimides. The required branched propargylic sulfides are prepared by an enantioselective organocatalytic aldehyde α-sulfenylation followed by Corey-Fuchs alkynylation.

Oxaziridine-mediated amination of branched allylic sulfides: Stereospecific formation of allylic amine derivatives via [2,3]-sigmatropic rearrangement

Reaction of branched allylic sulfides with the N-Bocoxaziridine 1 results in [2,3]-sigmatropic rearrangement of the intermediate allylic N-Boc-surfimides with a high level of chirality transfer. The first example of formation of a quaternary stereocenter