Title:
METHOD FOR PREPARING 2-FLUORO-2-METHYLDEOXYNUCLEOSIDE AS AN INTERMEDIATE OF SOFOSBUVIR
Document Type and Number:
WIPO Patent Application WO/2018/045997
Kind Code:
A1
Abstract:
The present application falls within the field of drug synthesis, and relates to a method for preparing 2-fluoro-2-methyldeoxynucleoside as an intermediate of Sofosbuvir. In particular, the present application provides a method for preparing a compound of formula V from a compound of formula II, and the intermediates used. The preparation method of the present application stereoselectively obtains the compound of formula V as β isomer in a condensation reaction, can be used for increasing the yield of a synthetic route of the intermediate of Sofosbuvir, i.e. the compound of formula 1, has a low process route cost and is more suitable for industrial scale-up.
Inventors:
KONG RUI (CN)
YUAN ZHEDONG (CN)
GUO MENG (CN)
HU MINGTONG (CN)
WANG DUZHENG (CN)
QIANG BIN (CN)
YUAN ZHEDONG (CN)
GUO MENG (CN)
HU MINGTONG (CN)
WANG DUZHENG (CN)
QIANG BIN (CN)
Application Number:
PCT/CN2017/101078
Publication Date:
March 15, 2018
Filing Date:
September 08, 2017
Export Citation:
Assignee:
SHANGHAI DUDE MEDICAL SCIENCE AND TECH CO LTD (CN)
CHIA TAI TIANQING PHARMACEUTICAL GROUP CO LTD (CN)
CHIA TAI TIANQING PHARMACEUTICAL GROUP CO LTD (CN)
International Classes:
C07H19/06; C07D307/33; C07D317/30; C07H1/00; C07H13/06
Domestic Patent References:
| WO2013178571A1 | 2013-12-05 | |||
| WO2011005860A2 | 2011-01-13 | |||
| WO2017077552A1 | 2017-05-11 |
Foreign References:
| CN106146585A | 2016-11-23 |
Other References:
MICHAEL, J. SOFIA ET AL.: "Discovery of a beta -D-20-Deoxy-20-r-fluoro-20- beta -C-methyluridin Nucleotide Prodrug (PSI-7977) for the Treatment of Hepatitis C Virus", JOURNAL OF MEDICINAL CHEMISTRY, vol. 53, no. 19, 16 September 2010 (2010-09-16), pages 7204 - 7218, XP055004442
Attorney, Agent or Firm:
LINDA LIU & PARTNERS (CN)
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