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    • 8. 发明公开
    • Synthesis of intermediates for the preparation of pramipexol
    • Herstellung von Pramipexol的Synthese von Zwischenproduktenfürdie
    • EP1808492A1
    • 2007-07-18
    • EP07000277.9
    • 2007-01-08
    • Dipharma Francis S.r.l.
    • Riva, SergioFassi, PaolaScarpellini, MicheleAllegrini, PietroRazzetti, Gabriele
    • C12P17/14C12P41/00C07D277/82
    • 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 R 1 is straight or branched C 1 -C 6 alkyl, optionally substituted with phenyl; and the asterisk * and R have the meanings 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)的酸作为单独的(R)对映异构体或(S)的酸的方法或其盐,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)对映异构体或其盐的混合物,其中R 1是直链或支链C 1 -C 6烷基,任选地 被苯基取代; 和星号*和R具有上述定义,与来自南极念珠菌的脂肪酶在有效获得包含式(I)的酸的混合物作为单独的(R)对映体的条件下,和式(II)的酯 ),作为个体(S)对映异构体; 随后水解后者以获得式(I)的酸作为个体(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。