Process for preparing scopine esters
    34.
    发明授权
    Process for preparing scopine esters 有权
    制备莨菪碱的方法

    公开(公告)号:US06747154B2

    公开(公告)日:2004-06-08

    申请号:US10339480

    申请日:2003-01-09

    IPC分类号: C07D45110

    CPC分类号: C07D451/10

    摘要: A process for preparing a compound of formula 1 from a compound of formula 2 the process comprising reacting in one step the compound of formula 2 with a compound of formula 3 wherein: X− is chlorine, bromine, iodine, methanesulfonate, or trifluoromethanesulfonate; R1 is hydroxy, C1-C4-alkyl, C1-C4-alkoxy, CF3, or fluorine; Ar is phenyl, naphthyl, thienyl, and furyl, each optionally mono- or disubstituted with one or two groups selected from C1-C4-alkyl, C1-C4-alkoxy, hydroxy, fluorine, chlorine, bromine, or CF3; Y− is chlorine, bromine, iodine, methanesulfonate, or trifluoromethanesulfonate; and R is hydroxy, methoxy, ethoxy, O—N-succinimide, O—N-phthalimide, phenyloxy, nitrophenyloxy, fluorophenyloxy, pentafluorophenyloxy, vinyloxy, 2-allyloxy, —S-methyl, —S-ethyl, or —S-phenyl.

    摘要翻译: 一种从式2化合物制备式1化合物的方法,该方法包括一步反应式2的化合物与式3的化合物,其中X 1是氯,溴,碘,甲磺酸酯或三氟甲磺酸酯; 1是羟基,C 1 -C 4 - 烷基,C 1 -C 4 - 烷氧基,CF 3或氟; Ar是苯基,萘基,噻吩基和呋喃基,各自任选被一个或两个选自C 1 -C 4 - 烷基,C 1 -C 4 - 烷氧基,羟基,氟,氯,溴或CF 3; Y 1是氯,溴,碘,甲磺酸酯或三氟甲磺酸酯; 和R是羟基,甲氧基,乙氧基,O-N-琥珀酰亚胺,O-N-邻苯二甲酰亚胺,苯氧基,硝基苯氧基,氟苯氧基,五氟苯氧基,乙烯基氧基,2-烯丙氧基,-S-甲基,-S-乙基或-S-苯基。

    Production method
    39.
    发明授权
    Production method 有权
    生产方式

    公开(公告)号:US07696346B2

    公开(公告)日:2010-04-13

    申请号:US11840397

    申请日:2007-08-17

    IPC分类号: C07D401/04 C07D401/14

    摘要: The present invention relates to a process for preparing compounds of general formula I wherein R1 and R2 are defined as in claim 1, the pharmaceutically acceptable salts and the solvates thereof, which may be prepared starting from compounds of general formula II wherein R1 is defined as in claim 1.

    摘要翻译: 本发明涉及一种制备通式Ⅰ化合物的方法,其中R 1和R 2如权利要求1所定义,其药学上可接受的盐和溶剂化物,其可以从通式II的化合物制备,其中R1定义为 在权利要求1中。