Title:
METHOD FOR PREPARING MOXIFLOXACIN INTERMEDIATE (S, S)-2, 8-DIAZABICYCLO [4, 3, 0] NONANE
Document Type and Number:
WIPO Patent Application WO/2022/166436
Kind Code:
A1
Abstract:
The present invention relates to the technical field of organic synthesis, and provides a method for preparing a Moxifloxacin intermediate (S, S)-2, 8-diazabicyclo [4, 3, 0] nonane. According to the present invention, azaphthalide is used as a raw material, and due to a cyclic structure of the azaphthalide itself, another two non-corresponding chiral isomers which are not required in chiral reduction are hardly generated, the chiral purity of the reduced intermediate itself is very high, resolution does not need to be performed again, and (S, S)-2, 8-diazabicyclo [4, 3, 0] nonane can be obtained directly by means of subsequent ammonolysis, reduction, chlorination, and cyclization. The method provided by the present invention does not need to perform chiral resolution, and has simple process, short process steps, low cost, high chiral purity of the product, and high total yield. Furthermore, in the subsequent steps of salifying and refining the product, a carboxylic acid containing a chiral structure is not required for salifying, so that the purity of the product can be further increased by performing refining with a common non-chiral carboxylic acid.
Inventors:
HAN DEMAN (CN)
LI YUNGUANG (CN)
WU CHENGLIN (CN)
HE JIAOJIAO (CN)
LI YUNGUANG (CN)
WU CHENGLIN (CN)
HE JIAOJIAO (CN)
Application Number:
PCT/CN2021/139394
Publication Date:
August 11, 2022
Filing Date:
December 18, 2021
Export Citation:
Assignee:
TAIZHOU BIOMEDICAL AND CHEMISTRY INDUSTRY RES INSTITUTE CO LTD (CN)
International Classes:
C07D471/04
Foreign References:
| CN112920184A | 2021-06-08 | |||
| CN112939847A | 2021-06-11 | |||
| CN112939849A | 2021-06-11 | |||
| IN202023007365A | 2021-08-27 | |||
| CN110317201A | 2019-10-11 | |||
| CN107686852A | 2018-02-13 | |||
| CN103044418A | 2013-04-17 | |||
| ITMI20090332A1 | 2010-09-07 |
Other References:
CHEN, ZHIWEI ET AL.: "Process Improvement on the Synthesis of (S,S)-2,8-diazabicyclo[4.3.0]nonane", CHINESE JOURNAL OF SYNTHETIC CHEMISTRY, vol. 21, no. 6, 31 December 2013 (2013-12-31), pages 760 - 762
Attorney, Agent or Firm:
BEIJING GAOWO LAW FIRM (CN)
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