Invention Grant
- Patent Title: Process for preparation of water-soluble azole prodrugs
- Patent Title (中): 制备水溶性唑前体药物的方法
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Application No.: US12097244Application Date: 2006-12-20
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Publication No.: US07803949B2Publication Date: 2010-09-28
- Inventor: Manabu Sasho , Keizo Sato , Jun Niijima , Mamoru Miyazawa , Shigeto Negi , Atsushi Kamada
- Applicant: Manabu Sasho , Keizo Sato , Jun Niijima , Mamoru Miyazawa , Shigeto Negi , Atsushi Kamada
- Applicant Address: JP Tokyo
- Assignee: Eisai R&D Management Co., Ltd.
- Current Assignee: Eisai R&D Management Co., Ltd.
- Current Assignee Address: JP Tokyo
- Agency: Birch, Stewart, Kolasch & Birch, LLP
- Priority: JP2005-366862 20051220; JP2006-032913 20060209
- International Application: PCT/JP2006/325352 WO 20061220
- International Announcement: WO2007/072851 WO 20070628
- Main IPC: C07F9/06
- IPC: C07F9/06

Abstract:
An object of the present invention is to provide a process, or the like, suitable for the industrialization of effective deprotection reaction without using a toxic solvent as well as to provide a process, or the like, for preparing a water-soluble azole prodrug effectively. The present invention provides a process for preparing a salt represented by Formula (I); (wherein X represents a fluorine atom bonded at position 4 or position 5 of a phenyl group) comprising the steps of: (a) carrying out a deprotection reaction of a compound represented by Formula (II); (wherein X represents a fluorine atom bonded at position 4 or position 5 of a phenyl group) in the presence of a carbocation scavenger.
Public/Granted literature
- US20090192316A1 PROCESS FOR PREPARATION OF WATER-SOLUBLE AZOLE PRODRUGS Public/Granted day:2009-07-30
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