利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

7 条记录 (耗时 0.015 秒)

    Process for the preparation of heterocyclic alkylamide derivatives
    2.
    发明授权
    Process for the preparation of heterocyclic alkylamide derivatives 失效
    制备杂环烷基酰胺衍生物的方法

    公开(公告)号：US5432284A

    公开(公告)日：1995-07-11

    申请号：US118073

    申请日：1993-09-08

    申请人： John H. Dygos ,  Thomas R. Kowar ,  Kathleen T. McLaughlin ,  Gatis Plume ,  Michael L. Prunier ,  Richard J. Salzmann ,  Mike G. Scaros ,  Joseph J. Wieczorek

    发明人： John H. Dygos ,  Thomas R. Kowar ,  Kathleen T. McLaughlin ,  Gatis Plume ,  Michael L. Prunier ,  Richard J. Salzmann ,  Mike G. Scaros ,  Joseph J. Wieczorek

    IPC分类号： C07D295/145 ,  C07D207/09 ,  C07D211/32 ,  C07D211/60

    CPC分类号： C07D295/145

    摘要： The present invention relates to a novel process for the preparation of heterocyclic alkylamide derivatives having the following formula: ##STR1## and the pharmaceutically acceptable acid addition salt thereof wherein X represents halo, alkyl having 1 to 6 carbon atoms, hydrido, trifluoromethyl, phenyl, or lower alkoxy having 1 to 6 carbon atoms; Y represents the group --CN or --CONH.sub.2 ; R.sub.2 represents alkyl having 1 to 6 carbon atoms; R.sub.3 represents acetyl, benzoyl, phenacetyl or trifluoroacetyl; m is the integer 1 or 2 and n is an integer from 1 to 3 inclusive; which comprises alkylating an aminoalkanol using a benzaldehyde/aminoalkanol/ketone mixture in the presence of a platinum catalyst to give an alkyl substituted phenylmethylaminoalkanol; halogenating the alkanol using a halogenating agent to give a haloalkyl alkylbenzenemethanamine salt; treating the salt with substituted phenyl piperidinealkanenitrile or substituted phenyl pyrrolidinealkanenitrile in the presence of base and dimethyl sulfoxide to give a substituted phenyl substituted aminoalkyl piperidinealkanenitrile or substituted aminoalkyl pyrrolidinealkanenitrile; hydration of the nitrile to give the corresponding amide; and N-debenzylation of the amide followed by acetylation to give the compounds of formula I wherein Y is --CONH.sub.2.

    摘要翻译： 本发明涉及制备具有下式的杂环烷基酰胺衍生物的新方法：其中X表示卤素，具有1至6个碳原子的烷基，羟基，三氟甲基（I）及其药学上可接受的酸加成盐 ，苯基或具有1至6个碳原子的低级烷氧基; Y代表基团-CN或-CONH 2; R 2表示具有1至6个碳原子的烷基; R3表示乙酰基，苯甲酰基，苯乙酰基或三氟乙酰基; m为1或2的整数，n为1〜3的整数， 其包括在铂催化剂存在下使用苯甲醛/氨基烷醇/酮混合物烷基化氨基烷醇，得到烷基取代的苯基甲基氨基烷基醇; 使用卤化剂卤化烷醇得到卤代烷基烷基苯甲胺盐; 在碱和二甲基亚砜的存在下用取代的苯基哌啶烷腈或取代的苯基吡咯烷烷腈处理盐，得到取代的苯基取代的氨基烷基哌啶烷腈或取代的氨基烷基吡咯烷烷腈; 腈水合得到相应的酰胺; 和酰胺的N-去苄基化，然后进行乙酰化，得到其中Y为-CONH 2的式I化合物。

    Process for the preparation of diethyl 2-]2-cyano-5-(dimethylamino)-2-(3-methoxyphenyl)-1,1-dimethylpentyl]prop andioate
    3.
    发明授权
    Process for the preparation of diethyl 2-]2-cyano-5-(dimethylamino)-2-(3-methoxyphenyl)-1,1-dimethylpentyl]prop andioate 失效
    制备2-] 2-氰基-5-（二甲基氨基）-2-（3-甲氧基苯基）-1,1-二甲基戊基]丙二酸二乙酯的方法

    公开(公告)号：US5220019A

    公开(公告)日：1993-06-15

    申请号：US859189

    申请日：1992-03-27

    申请人： John H. Dygos ,  Kathleen T. McLaughlin ,  John S. Ng ,  Kalidas Paul

    发明人： John H. Dygos ,  Kathleen T. McLaughlin ,  John S. Ng ,  Kalidas Paul

    IPC分类号： C07D211/88

    CPC分类号： C07D211/88

    摘要： Disclosed is a process for the preparation of 3-aryl-3-aminoalkyl-2,6-dioxohexahydropridines and particularly the compound 3-[3-(dimethylamino)propyl]3-(3 methoxyphenyl)-4, 4-dimethyl-2,6-piperidinedione, monohydrochloride, which is useful as an antidepressant.The process of the present invention comprises the condensation of a sterically hindered nitrile with a sterically hindered .alpha.,.beta.-unsaturated diester to produce a nitrile diester. These compounds can then undergo acid catalyzed cyclization and decarboalkoxylation in a one step process to provide the desired 3-aryl-3-aminoalkyl-2,6 -dioxohexahydropyridine.

    摘要翻译： 公开了制备3-芳基-3-氨基烷基-2,6-二氧代六氢吡啶的方法，特别是化合物3- [3-（二甲基氨基）丙基] -3-（3-甲氧基苯基）-4,4-二甲基-2- 6-哌啶二酮，一盐酸盐，其可用作抗抑郁药。 本发明的方法包括将空间位阻腈与空间位阻的α，β-不饱和二酯缩合以制备腈二酯。 然后这些化合物可以在一步法中进行酸催化环化和脱羰基烷氧基化，得到所需的3-芳基-3-氨基烷基-2,6-二氧代六氢吡啶。