| 摘要 |
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. |
| 主权项 |
1. A method for preparing an intermediate of R-praziquantel, represented by formula (4), comprising the step of hydrolyzing compound (2) by lipase at a temperature of 0-80° C. to obtain a compound of formula (4), an intermediate of R-praziquantel;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 subtilis, Fusarium solani pisi, Alcaligenes, Rhizopus niveus, Mucor Javanicus, Rhizopus Oryzae, and Fusarium solani (Mart.) Sacc. |
