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    • 3. 发明申请
    • PROCESS FOR THE PREPARATION OF ENANTIOMERICALLY PURE 1-SUBSTITUTED-3-AMINOALCOHOLS
    • 制备纯化1-取代的3-氨基醇的方法
    • WO2005080370A1
    • 2005-09-01
    • PCT/EP2005/001781
    • 2005-02-21
    • LONZA AGMICHEL, DominiqueMETTLER, HanspeterMCGARRITY, John
    • MICHEL, DominiqueMETTLER, HanspeterMCGARRITY, John
    • C07D333/20
    • C07C213/00C07B2200/07C07D333/22
    • Provided is a process for the preparation of enantiomerically pure 1-substituted-3-aminoalcohols, particularly of (S)-(-)- and (R)-(+)-3- N -methylamino-l-(2-thienyl)-1-propanol, by asymmetrically hydrogenating salts of a carboxylic acids with an aminoketone of formula (II), wherein R 1 is selected from the group consisting of 2-thienyl, 2-furanyl and phenyl, each optionally substituted with one or more halogen atoms and/or one or more C 1-4 -alkoxy groups, and wherein R 2 is C 1-4 -alkyl or phenyl, each optionally substituted with one or more halogen atoms and/or one or more C 1-4 -alkyl or C 1-4 -alkoxy groups, and wherein the corresponding aminoalcohols are obtained by subsequent hydrolysis of their salts. Furthermore provided are salts of a carboxylic acid with said aminoketones and the aminoalcohols obtained by asymmetriacally hydrogenating said aminoketones, respectively.
    • 提供了制备对映体纯的1-取代-3-氨基醇,特别是(S) - ( - ) - 和(R) - (+) - 3-N-甲基氨基-1-(2-噻吩基) -1-丙醇,通过用式(II)的氨基酮不对称氢化羧酸盐,其中R 1选自2-噻吩基,2-呋喃基和苯基,各自任选被一个或多个 更多的卤素原子和/或一个或多个C 1-4 - 烷氧基,并且其中R 2是C 1-4 - 烷基或苯基,各自任选被一个或多个卤素原子和/或一个或多个C 1-4 - 烷基或C 1-4 - 烷氧基,并且其中相应的氨基醇通过其盐的随后水解获得。 此外,还提供了羧酸与所述氨基酮和通过不对称地氢化所述氨基酮而获得的氨基醇的盐。