发明授权
US5034541A Method of preparing
1-phenyl-1-diethylaminocarbonyl-2-phthalimidomethyl-cyclopropane-z
失效
1-苯基-1-二乙基氨基羰基-2-邻苯二甲酰亚氨基甲基 - 环丙烷-z的制备方法
- 专利标题: Method of preparing 1-phenyl-1-diethylaminocarbonyl-2-phthalimidomethyl-cyclopropane-z
- 专利标题(中): 1-苯基-1-二乙基氨基羰基-2-邻苯二甲酰亚氨基甲基 - 环丙烷-z的制备方法
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申请号: US457352申请日: 1989-12-27
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公开(公告)号: US5034541A公开(公告)日: 1991-07-23
- 发明人: Dennis C. H. Bigg , Patrick Lesimple
- 申请人: Dennis C. H. Bigg , Patrick Lesimple
- 申请人地址: FRX Castres
- 专利权人: Pierre Fabre Medicament
- 当前专利权人: Pierre Fabre Medicament
- 当前专利权人地址: FRX Castres
- 优先权: FRX8817326 19881228
- 主分类号: C07D209/48
- IPC分类号: C07D209/48 ; C07D209/49
摘要:
A method of preparing 1-phenyl-1-diethylaminocarbonyl-2-phthalimidomethyl-cyclopropane-Z and key intermediates therefor are disclosed.This method is characterized by the following successive steps:opening of the 1-phenyl-2-oxo-3-oxa-bicyclo(3:1:0)-hexane by diethylamine or a tertiary amine with the aid of a Lewis acid/amine complex:the 1-phenyl-1-diethylaminocarbonyl-2-hydroxymethyl-cyclopropane-Z thus obtained is converted into a 2-chlorinated derivative by the action of a chlorination reagent such as thionyl chloride; andthe 1-phenyl-1-diethylaminocarbonyl-2-chloromethylcyclopropane-Z is reacted with a phthalimide salt in an organic solvent to produce the 1-phenyl-1-diethylaminocarbonyl-2-phthaliumidomethyl-cyclopropane-Z.
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