Title:
METHOD FOR IMPROVING SYNTHESIS PROCESS OF HYPIDONE FREE BASE
Document Type and Number:
WIPO Patent Application WO/2021/259051
Kind Code:
A1
Abstract:
Provided is a preparation method for improving the conversion of an improved hypidone free base, the method comprising reacting 2-hydroxypyridine and an epoxy represented by formula (I) under the action of a phase transfer catalyst and an inorganic base in an organic solvent, so as to obtain a hypidone free base as represented by formula (II). The preparation provided by the present invention greatly improves the reaction efficiency, reduces the reaction time, improves the reaction yield, and is very suitable for industrialized production.
Inventors:
WANG YOUGUI (CN)
CAI CHANGQING (CN)
GUO PAN (CN)
ZHU YUANXUN (CN)
YAN FENGFENG (CN)
CAI CHANGQING (CN)
GUO PAN (CN)
ZHU YUANXUN (CN)
YAN FENGFENG (CN)
Application Number:
PCT/CN2021/098608
Publication Date:
December 30, 2021
Filing Date:
June 07, 2021
Export Citation:
Assignee:
ZHEJIANG HUAHAI PHARM CO LTD (CN)
International Classes:
C07D401/06; A61K31/4545; A61P25/24
Foreign References:
| CN111747926A | 2020-10-09 | |||
| CN102241667A | 2011-11-16 | |||
| CN109134432A | 2019-01-04 | |||
| CN101429168A | 2009-05-13 | |||
| CN106588791A | 2017-04-26 |
Other References:
ABASS MOHAMED, AISHA S. MAYAS: "Substituted Pyridopyrimidinones, 1: Convenient PTC Alkylation and Halogenation of 2-hydroxy-4H-pyrido[1, 2-a]pyrimidin-4-one", HETEROATOM CHEMISTRY, vol. 18, no. 1, 3 January 2007 (2007-01-03), pages 19 - 27, XP055882679, DOI: 10.1002/hc.20245
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