Patent · US Active

Asymmetric synthesis method, related raw material and preparation method of (S,S)-2,8-diazabicyclo[4,3,0]nonane

US9238648B2 · kind B2 · utility

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3Claims

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Inventors

Xiaobo Shentu · Shanghai, CN
Yantao Qi · Shanghai, CN
Lingshi Xie · Shanghai, CN
Bo Wang · Tuji, CN

Key dates

Filing date	Sep 20, 2012
Grant date	Jan 19, 2016
Priority date	—
Expiry date	Sep 20, 2032

Classification

Technology area (CPC Y)Emerging Cross-Sectional Technologies
CPC primaryY02P20/55
WIPO fieldOrganic fine chemistry
WIPO sectorChemistry

Abstract

The present invention relates to an asymmetric synthesis method of a chiral intermediate (S,S)-2,8-diazabicyclo[4,3,0]nonane (I) of moxifloxacin, wherein an imide or enamine compound is obtained by dehydration reaction of the pyrrolidine-3-ketone as shown in formula (II) and chiral amine(R)-1-phenylethylamine, followed by the reduction of the imide or enamine compound to obtain a compound of formula (III) or (IV) having the chiral structure of formula (I), and then a compound of formula (I) is obtained by intramolecular cyclization, and removal of the chiral auxiliary group and amino-protecting group. The present invention also relates to pyrrolidine-3-ketone as shown in formula (II) and a preparation method therefor,

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.