Invention Grant
- Patent Title: Process for preparation of temsirolimus
- Patent Title (中): 替西罗莫司的制备方法
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Application No.: US12661928Application Date: 2010-03-29
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Publication No.: US08258299B2Publication Date: 2012-09-04
- Inventor: Kwang-Chung Lee , Ting-Huei Lee , Yen-Shih Tung , Chia-Chen Kao , Tzu-Ai Lee
- Applicant: Kwang-Chung Lee , Ting-Huei Lee , Yen-Shih Tung , Chia-Chen Kao , Tzu-Ai Lee
- Applicant Address: TW New Taipei
- Assignee: Chungwa Chemical Synthesis & Biotech Co., Ltd.
- Current Assignee: Chungwa Chemical Synthesis & Biotech Co., Ltd.
- Current Assignee Address: TW New Taipei
- Priority: TW98110170A 20090327
- Main IPC: C07D491/12
- IPC: C07D491/12 ; C07D498/12

Abstract:
The present invention provides two synthetic routes for the preparation of Temsirolimus (compound 1b and analog of Temsirolimus 1a). The first route includes the synthesis of CCI-779 by directly reacting rapamycin (4b) or Prolyl-rapamycin (4a) with substituent-2,2-bis(methoxy) propionic acid anhydride(11) in the presence of an organic base, followed by deprotection to give CCI-779 or Proline CCI-779. The second route includes a process involving a reaction of rapamycin-OH-31-sily ether (4d) or Prolyl-rapamycin-OH-31-sily ether (4c) with substituent-2,2-bis(methoxy) propionic acid anhydride(11) in the presence of an organic base and followed by subsequent hydrolysis step to obtain the desired CCI-779 or Proline CCI-779.Compound 11, as described in this invention, is stable at room temperature, cost effective and ease of processing.
Public/Granted literature
- US20100249415A1 Process for preparation of temsirolimus Public/Granted day:2010-09-30
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