Gannex Pharma Co., Ltd.

Shanghai Institute of Pharmaceutical Industry

Zhejiang Hisun Pharmaceutical Co., Ltd.

China National Medicines Guorui Pharmaceutical Co., Ltd.

Bin Liang

Jinzi Jason Wu

Bailing Yang

Fuli Zhang

Chunbo Yang

Yang Gao

Jian Chai

Jiang Li

Jian Wang

Pengcheng Qiu

Hairong Luo

Qingfeng Cai

Chonghao Liu

Min Jiang

A method for preparing the cyclic phosphonate compound of Formula I is described. The method significantly improves the stereoselectivity of the compound with the required configuration.

Preparation method of a cyclic phosphonate compound

Disclosed is a new method for preparing a methyl substitute of a linezolid intermediate, (S)-2-(3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazoline) (I), wherein the intermediate (I) is obtained by the cyclization of 3-fluoro-4-morpholinophenyl isocyanate (II) and epoxy compound (III). This process has a short process route, low cost, easy operation, and high yield, so is suitable for a large-scale industrial production. 

Method for preparing linezolid intermediate

A method for preparing a Rivaroxaban intermediate I is presented, including the following step: in a non-protonic solvent, under the effect of lewis acid, performing cyclization reaction on 4-(4-phenyl isocyanate)morpholine-3-ketone (II) and (S)-epoxy compound (III), the reaction temperature ranging from 20&#xb0; C. to 60&#xb0; C., where R is amino replaced by amino protecting group. The preparation method of the present invention has a mild condition, a simple process, a low cost, and high efficiency; the product is easy to purify and the method is applicable to industrial production.

Method for preparing rivaroxaban intermediate

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Shanghai, China

Bin Liang