| 发明名称 |
PROCESS FOR PREPARING LEVOMILNACIPRAN HCL |
| 摘要 |
The invention relates to one-pot process for preparing (1S,2R)-1-phenyl-1-(N,N-diethylaminocarbonyl)-2-aminomethylcyclopropane of formula (I) comprising the step of reacting (1S,2R)-N,N-diethyl-2-(hydroxymethyl)-1-phenylcyclopropanecarboxamide successively with the following reactants 1) triethyl orthoformate and methanesulfonic acid or triethylamine and methanesulfonyl chloride, 2) a phthalimidating agent, 3) aqueous EtNH2, wherein the reaction is carried out in toluene. In another aspect the invention concerns a process for preparing (1S,2R)-N,N-diethyl-2-(hydroxymethyl)-1-phenylcyclopropanecarboxamide trough a step of crystallization of (1S,5R)-1-phenyl-3-oxabicyclo[3.1.0]hexan-2-one. |
| 申请公布号 |
US2014343322(A1) |
申请公布日期 |
2014.11.20 |
| 申请号 |
US201414282554 |
申请日期 |
2014.05.20 |
| 申请人 |
COSMA S.P.A. |
发明人 |
CELESTINI Paolo;BARETTI Sergio;PIZZATTI Enrica |
| 分类号 |
C07C231/12 |
主分类号 |
C07C231/12 |
| 代理机构 |
|
代理人 |
|
| 主权项 |
1. A one-pot process for preparing (1S,2R)-1-phenyl-1-(N,N-diethylaminocarbonyl)-2-aminomethylcyclopropane of formula (I)comprising the step of reacting (1S,2R)-N,N-diethyl-2-(hydroxymethyl)-1-phenylcyclopropanecarboxamide successively with the following reactants 1) triethyl orthoformate and methanesulfonic acid or triethylamine and methanesulfonyl chloride, 2) a phthalimidating agent, 3) aqueous EtNH2,wherein the reaction is carried out in toluene. |
| 地址 |
Ciserano IT |
