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    • 1. 发明申请
    • PROCESS FOR PREPARING 2-AMINOTHIAZOL-4-YL-ACETIC ACID DERIVATES
    • 制备2-氨基四氢-4-戊酸衍生物的方法
    • WO2011029596A1
    • 2011-03-17
    • PCT/EP2010/005538
    • 2010-09-09
    • LONZA LTDDAI, DanmeiZHU, WeiWANG, Siming
    • DAI, DanmeiZHU, WeiWANG, Siming
    • C07D277/38A61K31/426
    • C07D277/40
    • The invention provides a process for preparing a (2-aminothiazol-4-yl)-triarylmethyloxy- iminoacetic acid of the formula (I) or an ester thereof of the formula (II) wherein R 1 , R 2 and R 3 independently are optionally substituted phenyl groups and R 4 is C 1-6 alkyl, by reacting a (2-aminothiazol-4-yl)hydroxyiminoacetic acid ester of the formula (III) wherein R 4 is as defined above, with an alcohol of the formula R 1 R 2 R 3 COH, wherein R 1 , R 2 and R 3 are as defined above, in the presence of BF 3 to form a (2-aminothiazol-4-yl)triaryl-methyloxyiminoacetic acid ester of the formula (II), and, optionally, hydrolyzing said ester of formula (II) to obtain the acid of formula (I).
    • 本发明提供了制备式(I)的(2-氨基噻唑-4-基) - 三芳基甲氧基 - 亚氨基乙酸或其式(II)的酯的方法,其中R 1,R 2和R 3独立地是任选取代的苯基 和R 4是C 1-6烷基,其中R 4如上定义的式(III)的(2-氨基噻唑-4-基)羟基亚氨基乙酸酯与式R 1 R 2 R 3 COH的醇反应,其中R1,R2和R3 在BF 3存在下形成式(II)的(2-氨基噻唑-4-基)三芳基 - 甲氧基亚氨基乙酸酯,和任选地水解所述式(II)的酯以获得酸 的式(I)化合物。