41029-80-5Relevant academic research and scientific papers
Tailored sol-gel immobilized lipase preparates for the enzymatic kinetic resolution of heteroaromatic alcohols in batch and continuous flow systems
Moisǎ, Mǎdǎlina Elena,Spelmezan, Cristina Georgiana,Paul, Cristina,Bartha-Vári, Judith Hajnal,Bencze, László Csaba,Irimie, Florin Dan,Paizs, Csaba,Péter, Fráncisc,To?a, Monica Ioana
, p. 52977 - 52987 (2017/11/24)
Tailored immobilized lipases from Candida antarctica B and Pseudomonas fluorescens, with improved thermal and operational stability, were prepared through fine tuning of the structure of the sol-gel matrix, using various binary or ternary precursor mixtures for the EKR of various chiral heteroaromatic secondary alcohols with benzofuran, benzo[b]thiophen, phenothiazine and 2-phenylthiazol moieties. The operational stability in batch process was studied for five selected systems by performing reuse experiments, using the conversion, enantiomeric excesses and enantiomeric ratio as parameters, demonstrating the dependence of the sol-gel lipase preparate performance on the structure of both biocatalyst and substrate. The resolution of the benzofuranic substrates with the best performing biocatalysts was studied in continuous-flow mode, using the productivity as a criterion. The specific reaction rates under continuous-flow operation (rflow) were higher than those obtained in batch mode (rbatch) in both cases, sustaining its usefulness for further process development.
Candida antarctica lipases acting as versatile catalysts for the synthesis of enantiopure (R)- and (S)-1-(2-phenylthiazol-4-yl)ethanamines This paper is dedicated to the anniversary of 95th birthday of Professor Valer Fǎrcǎ?anu.
Radu, Alexandra,Moisǎ, Mǎdǎlina Elena,To?a, Monica Ioana,Dima, Norbert,Zaharia, Valentin,Irimie, Florin Dan
, p. 114 - 119 (2014/07/08)
The synthesis of both enantiomers of four new phenylthiazole-based amines by enantiomer-selective acylation of racemic amines and by hydrolysis of the corresponding racemic amides using lipase B from Candida antarctica (Novozyme 435) as chiral catalyst was performed with good yields and excellent enantioselectivities. In order to prevent the frequently occurring partial racemization of enantiopure amides during chemical hydrolysis to the corresponding (R)-amines, the deprotection of the N-acylated (R)-enantiomers by mild enzymatic hydrolysis with lipase A from C. antarctica immobilized on Celite was also developed.
Heterocycles 32. Efficient kinetic resolution of 1-(2-arylthiazol-4-yl) ethanols and their acetates using lipase B from Candida antarctica
Hapau, Denisa,Brem, Juergen,Moisa, Madalina,Tosa, Monica-Ioana,Irimie, Florin Dan,Zaharia, Valentin
, p. 88 - 94 (2013/10/22)
In this paper we describe the chemoenzymatic synthesis of new enantiomerically enriched (R)- and (S)-1-(2-arylthiazol-4-yl)ethanols and their acetates by enzymatic enantioselective acetylation of the racemic alcohols rac-2a-d and by methanolysis of the corresponding racemic esters rac-3a-d mediated by lipase B from Candida antarctica (CaL-B) in non-aqueous media. In terms of stereoselectivity and activity, both procedures, acylation and alcoholysis, gave similar good results (50% conversion, E 〉 200). The absolute configuration of the kinetic resolution products was determined by a detailed 1H NMR study of the Mosher's derivatives of (S)-2b.
IMIDAZOTHIADIAZOLE AND IMIDAZOPYRAZINE DERIVATIVES AS PROTEASE ACTIVATED RECEPTOR 4 (PAR4) INHIBITORS FOR TREATING PLATELET AGGREGATION
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, (2013/11/18)
The present invention provides thiazole compounds of Formula I wherein W, Y, R0, R2, R4, R5, R6, R7, X1, X2, X3 and X4 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments for treating or preventing thromboembolic disorders.
