Method for preparing chiral disubstituted or alpha, alpha''-double instituted N-acylpyrrolidine or N-acylpiperidine
Title：
Method for preparing chiral disubstituted or alpha, alpha''-double instituted N-acylpyrrolidine or N-acylpiperidine
Application Number：
 200510123756
Application Date：
 2005/11/22
Announcement Date：
 2006/06/21
Pub. Date：
Publication Number：
 1789247
Announcement Number：
Grant Date：
Granted Pub. Date：
ApplicationType：
 Invention
State/Country：
 11[China|beijing]
IPC：
 C07D 211/10, C07D 207/06
Applicant(s)：
 Tsinghua University
Inventor(s)：
 Hu Yuefei, Wang Xinyan, Dong Yanmei, Liu Bo
Key Words：
 chiral disubstituted, alpha, alpha''-double instituted, N-acylpyrrolidine, N-acylpiperidine
Abstract：
 The invention discloses a method for preparing chirality ¦Á-substituent or ¦Á,¦Á'-bi substituent N-acylpyrrolidine or N-acylpiperidine, comprising the following steps: 1) making the compound in formula I react with organic metallic agent in orgain dissolvent, and getting compound of formula II, III or IV; the organic metallic agent is RMg or Rli; the organic dissolvent is ether, toluene, tetrahydrofuran or mixture of them; the reating temperature is from 0 to the boiling point of all organic dissolvent; 2) making compound of formula II, III or IV react with carboxyl acid, the said carboxyl acid reacting with acid anhydride and getting the said chirality ¦Á-substituent or ¦Á,¦Á'-bi substituent N-acylpyrrolidine or N-acylpiperidine. The invention is characterized by the simple reaction condition, high stereospecificity, high productivity of reaction product and suitness for mass production, which can not only get pyrrolidine compound and piperidine compound substituted by alkane, but also can get pyrrolidine compound and piperidine compound substituted by alkene.
Claim：
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2008-4-17
  Selected patents owned by Tsinghua University filed in 2005 are loaded.
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