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    • 8. 发明授权
    • Method for the preparation of citalopram
    • 西酞普兰制备方法
    • US06768011B2
    • 2004-07-27
    • US10232994
    • 2002-08-29
    • Michael Harold RockHaleh Ahmadian
    • Michael Harold RockHaleh Ahmadian
    • C07D30798
    • C07D307/87A61K31/343
    • The invention relates to a method for the preparation of citalopram comprising reaction of a compound of formula II with a compound having the formula wherein R is halogen or —O—SO2—X, wherein X is alkyl, alkenyl, alkynyl or optionally alkyl substituted aryl or aralkyl, and R1 is dimethylamino, halogen, —O—SO2—X wherein X is as defined above, provided that R is not halogen when R1 is dimethylamino; and if R1 is dimethylamino followed by isolation of citalopram base or a pharmaceutically acceptable acid addition salt thereof, and if R1 is halogen or —O—SO2—X, wherein X is as defined above, followed by conversion of the resulting compound of formula wherein R2 is halogen or a group of formula —O—SO2—X wherein X is as defined above to citalopram, followed by isolation of citalopram base or a pharmaceutically acceptable acid addition salt thereof.
    • 本发明涉及一种制备西酞普兰的方法,包括式II化合物与具有式R的化合物的反应:R为卤素或-O-SO 2 -X,其中X为烷基,烯基,炔基或任选的烷基取代的芳基或芳烷基 R 1是二甲基氨基,卤素,-O-SO 2 -X(其中X如上所定义),条件是当R 1是二甲基氨基时R不是卤素;如果R 1是二甲基氨基,然后分离 西酞普兰碱或其药学上可接受的酸加成盐,并且如果R 1是卤素或-O-SO 2 -X,其中X如上所定义,然后转化所得化合物的R 2是卤素或 式为-O-SO 2 -X的基团,其中X如上定义为西酞普兰,然后分离西酞普兰碱或其药学上可接受的酸加成盐。