Invention Grant
- Patent Title: Process for preparing 2′-deoxy-2′, 2′-difluorocytidine
- Patent Title (中): 制备2'-脱氧-2',2'-二氟胞苷的方法
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Application No.: US12532331Application Date: 2008-03-20
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Publication No.: US07994310B2Publication Date: 2011-08-09
- Inventor: Su-Jin Park , Chun-Rim Oh , Young-Deuck Kim
- Applicant: Su-Jin Park , Chun-Rim Oh , Young-Deuck Kim
- Applicant Address: KR Chungcheonbuk-Do
- Assignee: Dongwoo Syntech Co., Ltd.
- Current Assignee: Dongwoo Syntech Co., Ltd.
- Current Assignee Address: KR Chungcheonbuk-Do
- Agency: Lucas & Mercanti, LLP
- Priority: KR10-2007-0028526 20070323; KR10-2007-0128809 20071212
- International Application: PCT/KR2008/001566 WO 20080320
- International Announcement: WO2008/117955 WO 20081002
- Main IPC: C07H19/073
- IPC: C07H19/073

Abstract:
Disclosed is a method for preparing 2′-deoxy-2′,2′-difluorocytidine of Formula I comprising, preparing an optically pure 3R-hydroxypropane amide compound of Formula VIII from an optical ester compound of Formula IX using an optically active chiral amine, preparing an optically pure D-erythro-2,2-difluoro-2-deoxy-1-oxoribose compound of Formula V from the compound of Formula VIII, glycosylating the compound of Formula V with a nucleobase to prepare the 2′-deoxy-2′,2′-difluorocytidine of Formula I as a β-nucleoside. With the present invention, it is possible to prepare an optically pure compound of Formula I in a high purity and a high yield. In the Formulae, R1 and R2 are protecting groups and are each independently benzoyl, 4-methylbenzoyl, 3-methylbenzoyl, 4-cyanobenzoyl, 3-cyanobenzoyl, 4-propylbenzoyl, 2-ethoxybenzoyl, 4-t-butylbenzoyl, 1-naphthoyl or 2-naphthoyl, R3, R4 and R7 are each independently C1-C3 alkyl, R5 is methyl or ethyl, R6 is hydrogen, methyl or methoxy.
Public/Granted literature
- US20100069625A1 PROCESS FOR PREPARING OF 2'-DEOXY-2'2'-DIFLUOROCYTIDINE Public/Granted day:2010-03-18
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