Title:
PROCESS FOR PREPARING 2'-DEOXY-2',2'-DIFLUORO-β-CYTIDINE HYDROCHLORIDE
Document Type and Number:
WIPO Patent Application WO/2009/030075
Kind Code:
A1
Abstract:
The invention discloses a stereoselective process for preparing 2'-deoxy-2',2'-difluoro-β-cytidine hydrochloride (a compound of formula I), which comprises: 1) a compound of formula II is reacted with sodium halide to obtain a mixture of a compound of formula III and a compound of formula IV; 2) the mixture of step 1) is reacted with protected cytosine to obtain a compound of formula V; 3) the compound of formula V is deproteced and salted to form the compound of formula I. The specific reaction scheme is shown as following: In the process of the invention, the materials are cheap, the intermediates can be used without isolation, and the conversion of materials is significantly improved. Thus, the cost of production is largely decreased and the operation is simple. Therefore, the process is suitable for the industrial production.
Inventors:
LI JINLIANG (CN)
HUANG HONGJUN (CN)
LV FENG (CN)
HUANG HONGJUN (CN)
LV FENG (CN)
Application Number:
PCT/CN2007/003072
Publication Date:
March 12, 2009
Filing Date:
October 29, 2007
Export Citation:
Assignee:
SHANGHAI DESANO PHARMACEUTICAL (CN)
SHANGHAI DESANO CHEMICAL PHARM (CN)
LI JINLIANG (CN)
HUANG HONGJUN (CN)
LV FENG (CN)
SHANGHAI DESANO CHEMICAL PHARM (CN)
LI JINLIANG (CN)
HUANG HONGJUN (CN)
LV FENG (CN)
International Classes:
C07H19/073
Domestic Patent References:
| WO2006071090A1 | 2006-07-06 | |||
| WO2006011713A1 | 2006-02-02 |
Foreign References:
| CN101024667A | 2007-08-29 |
Attorney, Agent or Firm:
SHANGHAI L & W INTELLECTUAL PROPERTY LAW OFFICE, LLC (Suite 4A543 Xin Hua Road, Shanghai 2, CN)
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