6212-32-4

Upstream product

• 104-88-1 4-chlorobenzaldehyde 
• 124-38-9 carbon dioxide 
• 13312-83-9 4-chloromandelonitrile 
• 151-50-8 potassium cyanide 
• 506-87-6 ammonium carbonate 

Downstream Products

• 6212-33-5 2-(4-Chlorophenyl)glycine 
• 92874-70-9 DL-Benzyloxycarbonylamino-<4-chlor-phenyl>-essigsaeure 
• 126746-12-1 DL-2-(p-Chlorphenyl)glycinoctylesterhydrochlorid 
• 131402-93-2 Amino-(4-chloro-phenyl)-acetic acid heptyl ester; hydrochloride 
• 131402-92-1 Amino-(4-chloro-phenyl)-acetic acid hexyl ester; hydrochloride 
• 170119-35-4 Acetic acid {[1-(4-chloro-phenyl)-2-pyrrolidin-1-yl-ethyl]-methyl-carbamoyl}-(3,4-dichloro-phenyl)-methyl ester 
• 170119-40-1 [1-(4-Chloro-phenyl)-2-oxo-2-pyrrolidin-1-yl-ethyl]-carbamic acid methyl ester 
• 170119-37-6 (4-Chloro-phenyl)-methoxycarbonylamino-acetic acid 
• 170119-33-2 [1-(4-Chloro-phenyl)-2-pyrrolidin-1-yl-ethyl]-methyl-amine 

Relevant academic research and scientific papers

Method for continuously and quickly preparing DL-phenylglycine and analogue thereof

The invention provides a method for continuously and quickly preparing DL-phenylglycine and an analogue thereof. The method comprises the steps of adding 2-hydroxyl-phenylacetonitrile and an analoguethereof (cyanohydrin for short) and an aqueous ammonium bicarbonate solution into a microchannel reactor for a reaction, controlling the reaction temperature to be 80-130 DEG C, and controlling the reaction pressure to be 0.5-2.0 MPa, wherein the standing time of the reactants in a microchannel is 1-8 min, and an aqueous solution of 5-phenyl-hydantoin and an analogue thereof (hydantoin for short)is obtained; adding the hydantoin and alkali into the microchannel reactor for a reaction, controlling the reaction temperature to be 120-200 DEG C, and controlling the reaction pressure to be 1.0-3.5MPa, wherein the standing time of the reactants in the microchannel is 1-8 min, and then a saline solution of phenylglycine and an analogue thereof is obtained; conducting acidification neutralization and crystallization to obtain the phenylglycine and the analogue thereof. According to the method, the microchannel reactor is adopted, the reaction time is greatly shorted, the reaction speed is increased, pyrolysis and polymerization of the cyanohydrin are reduced, no by-products are generated, the products are high in yield, clean and environmentally friendly, and the production cost is lowered.

Benzimidazoles having antithrombotic activity

The present invention relates to new benzimidazoles of general formula whereinRa to Rc, A, Ar and B are defined as in claim 1, the tautomers, the stereoisomers, the mixtures thereof the prodrugs, the derivatives thereof which contain

Production of ring-substituted D-phenylglycines by microbial or enzymatic hydrolysis/deracemisation of the corresponding DL-hydantoins

A series of 17 ring-mono and -disubstituted D-phenylglycine derivatives was prepared in high enantiomeric purity by enzymatic hydrolysis and deracemisation of the corresponding DL-hydantoins, using D-hydantoinase activities of microorganisms or purified enzymes, followed by diazotation of the resulting N-carbamyl-D-amino acids. No significant L-hydantoinase activity was found to produce the corresponding L-enantiomers.

Synthesis and κ binding affinity of 1-(pyrrolidin-1-ylmethyl)-2-(N-methyl)-4--1,2,3,4-tetrahydroisoquinolin-3(2H)-ones

Diastereomeric forms of 1-(pyrrolidin-1-ylmethyl)-2-(N-methyl)-4--1,2,3,4-tetrahydroisoquinolin-3-(2H)-ones 3a and its chloro analog 3c were synthesized.Compounds 3a,c are related to the κ-selective opiate ICI 199441 1 by linking the benzylic CH2 to the ortho position of the phenyl in 1.Compared with morphine, these compounds had lost in κ and μ affinities; only cis-3a showed a modest κ affinity. 1-Pyrrolidin-1-ylmethyl-N--1,2,3,4-tetrahydroisoquinoline 2, which is also a cyclic congener of 1, was reported to display high κ and μ affinity, and so a conformational study was undertaken on 1, 2 and 3a.This showed that while active 2 extensively superposed on 1, 3a assumes another geometry which does now allow a fit with the pharmacophoric moieties of 1 and 2. tetrahydroisoquinolin-3(2H)-one / κ-opiate receptor / rigid congener