Enzymatic resolution of aryl and thio-substituted acids
    1.
    发明授权
    Enzymatic resolution of aryl and thio-substituted acids 失效
    芳基和硫取代的酸的酶解

    公开(公告)号:US07026143B2

    公开(公告)日:2006-04-11

    申请号:US10625404

    申请日:2003-07-23

    IPC分类号: C12P11/00

    摘要: Provided is a method of resolving a racemic mixture of a compound of formula I to obtain a desired enantiomer: wherein Ar is C6 or C10 aromatic group that can be substituted with H, C1 to C6 alkyl, trifluoromethyl or halo, R5 is halo or —S—R1, wherein R1 is H or acetyl, and R2 is H or C1 to C6 alkyl, the method comprising: reacting a compound of formula I wherein the compound is an ester whereby R2 is C1 to C6 alkyl with a lipase derived from Mucor meihei to stereoselectively hydrolyze the ester bond to produce an acid; and isolating the acid, wherein the reaction is conducted in a solvent comprising 80% to 98% v/v % organic phase and a residue of water phase (which can be buffered).

    摘要翻译: 提供了一种拆分式I化合物的外消旋混合物以获得所需对映异构体的方法:其中Ar是可以被取代的C 6或C 10芳族基团 H,C 1至C 6烷基,三氟甲基或卤素,R 5是卤素或-SR 1, 其中R 1是H或乙酰基,R 2是H或C 1 -C 6烷基,其中R 1是H或乙酰基,R 2是H或C 1 -C 6烷基, 方法包括:使式I化合物,其中所述化合物是酯,其中R 2是C 1 -C 6烷基与脂肪酶衍生的 从Mucor meihei到立体选择性地水解酯键以产生酸; 并分离酸,其中反应在包含80%至98%v / v%有机相和水相残余物(可缓冲)的溶剂中进行。