Invention Grant
- Patent Title: Process for the preparation of letrozole
- Patent Title (中): 来曲唑的制备方法
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Application No.: US11482228Application Date: 2006-07-06
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Publication No.: US07705159B2Publication Date: 2010-04-27
- Inventor: Peter Lindsay MacDonald , Ettore Bigatti , Pierluigi Rossetto , Zvi Harel
- Applicant: Peter Lindsay MacDonald , Ettore Bigatti , Pierluigi Rossetto , Zvi Harel
- Applicant Address: US CA Irvine
- Assignee: Sicor, Inc.
- Current Assignee: Sicor, Inc.
- Current Assignee Address: US CA Irvine
- Agency: Kenyon & Kenyon LLP
- Main IPC: C07D249/08
- IPC: C07D249/08

Abstract:
The invention provides a high-yield process for the preparation of letrozole having a high purity, without the need for removal of the 4-[1-(1,3,4-triazolyl)methyl]benzonitrile impurity at the intermediate stage. The invention also provides a process for the synthesis of letrozole in which formation of the impurity 4-[1-(1,3,4-triazolyl)methyl]benzonitrile during the first stage is minimized. In the process, a 4-(halomethyl)benzonitrile is reacted with a salt of 1H-1,2,4-triazole, reducing the formation of the impurity. Preferably, the preparation is conducted as a one-pot process.
Public/Granted literature
- US20070066831A1 Process for the preparation of letrozole Public/Granted day:2007-03-22
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