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    • 26. 发明申请
    • SYNTHESIS OF INTERMEDIATES FOR THE PREPARATION OF PRAMIPEXOL
    • 合成制备PRAMIPEXOL的中间体
    • US20070166814A1
    • 2007-07-19
    • US11622259
    • 2007-01-11
    • Sergio RIVAPaola FassiMichele ScarpelliniPietro AllegriniGabriele Razzetti
    • Sergio RIVAPaola FassiMichele ScarpelliniPietro AllegriniGabriele Razzetti
    • C12P41/00
    • C12P17/14C07D277/82C12P41/005
    • A process for the preparation of an acid of formula (I), as the individual (R) enantiomer or (S), or a salt thereof wherein R is a protected amino group; and the asterisk * denotes the stereogenic carbon atom, comprising contacting an ester of formula (II), as mixture of (R, S) enantiomers, or a salt thereof, wherein R1 is straight or branched C1-C6 alkyl, optionally substituted with phenyl; the asterisk * and R defined above), with a lipase from Candida antarctica, under conditions effective to obtain a mixture comprising an acid of formula (I), as the individual (R) enantiomer, and an ester of formula (II), as the individual (S) enantiomer; the subsequent hydrolysis of the latter to obtain an acid of formula (I), as the individual (S) enantiomer; and, if desired, the conversion of an acid of formula (I), either as the (R) or (S) enantiomer, to a salt thereof.
    • 制备式(I)的酸作为单个(R)对映异构体或(S)的方法或其盐,其中R是被保护的氨基; 并且星号*表示立体碳原子,包括使式(II)的酯作为(R,S)对映体或其盐的混合物,其中R 1是直链或支链C 任选被苯基取代的C 1 -C 6烷基; 在有效获得包含式(I)的酸的混合物作为单独的(R)对映异构体和式(II)的酯的混合物的条件下,将来自南极念珠菌的脂肪酶与式(II)的酯作为 个体(S)对映体; 随后水解后者以获得式(I)的酸作为单独的(S)对映异构体; 如果需要,将式(I)的酸作为(R)或(S)对映异构体转化为其盐。