Invention Grant
- Patent Title: Process for preparing voriconazole by using new intermediates
- Patent Title (中): 使用新中间体制备伏立康唑的方法
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Application No.: US13577055Application Date: 2011-02-01
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Publication No.: US08575344B2Publication Date: 2013-11-05
- Inventor: Hyuk Chul Kwon , Man Dong Rho , Kyung Hoi Cha
- Applicant: Hyuk Chul Kwon , Man Dong Rho , Kyung Hoi Cha
- Applicant Address: KR Seoul
- Assignee: Dongkook Pharmaceutical Co., Ltd.
- Current Assignee: Dongkook Pharmaceutical Co., Ltd.
- Current Assignee Address: KR Seoul
- Agency: Edwards Wildman Palmer LLP
- Priority: KR10-2010-0010467 20100204
- International Application: PCT/KR2011/000689 WO 20110201
- International Announcement: WO2011/096697 WO 20110811
- Main IPC: C07D403/06
- IPC: C07D403/06

Abstract:
Provided is a process for preparing Voriconazole represented by Chemical Formula 1. More particularly, the process for preparing Voriconazole of Chemical Formula 1 includes: carrying out the Reformatsky-type coupling reaction between a ketone derivative of Chemical Formula 4 and a pyrimidine derivative of Chemical Formula 5 to obtain a compound of Chemical Formula 3; reacting the substituents halo and oxysulfonyl with a hydrogen donor to obtain racemic Voriconazole of Chemical Formula 2; and carrying out optical isolation of the racemic Voriconazole by adding an adequate optically active acid thereto to obtain Voriconazole having high optical purity with high cost-efficiency and high yield.
Public/Granted literature
- US20130005973A1 PROCESS FOR PREPARING VORICONAZOLE BY USING NEW INTERMEDIATES Public/Granted day:2013-01-03
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