R-praziquantel preparation method
AssigneeSuzhou Tongli Biomedical Co., Ltd.
InventorMingxin Qian
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Abstract
Provided are R-praziquantel preparation methods, which utilize the characteristics of biological enzyme of strong stereoselectivity, site-selectivity, and regioselectivity, of high resolution efficiency, of mild reaction conditions, and of simple operations to catalyze the hydrolysis of a certain enantiomer in a chemically synthesized racemate or a derivative, thus acquiring a mixture of reacted and unreacted optical isomers. R-praziquantel prepared by the method can have a purity of 98% or more.
Claims10
A method for preparing an intermediate for the synthesis of R-praziquantel, of formula (4), comprising contacting compound (2) with a lipase in a reaction mixture at a temperature of 0-80°C. to obtain compound of formula (4);
- wherein the lipase comprises one or more lipases derived from Aspergillus niger, Candida rugosa, Rhizomucor miehei, Candida antarctica, Pseudomonas cepacia, Pseudomonas fluorescens, Thermomyces lanuginose, Bacillus subtillis, Fusarium solani pisi, Alcaligenes spp., Rhizopus niveus, Mucor javanicus, Rhizopus oryzae, and Fusarium solani (Mart.) sacc.
Dependencies are inferred from the claim text.