Shanghai Institute of Pharmaceutical Industry

Zhejiang Hisun Pharmaceutical Co., Ltd.

China National Medicines Guorui Pharmaceutical Co., Ltd.

Chunbo Yang

Fuli Zhang

Bin Liang

Yang Gao

Hua Bai

Zhiqing Yang

Jian Chai

Jiang Li

Zhezhou Yang

Jian Wang

Qingfeng Cai

Pengcheng Qiu

Hairong Luo

Chonghao Liu

Daoxin Chen

Rentong Sun

Min Jiang

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

The present invention provides a preparation method for (S)-3-(1-(dimethylamino)ethyl)phenyl ethyl(methyl)carbamate, preparation methods for intermediates (S)-1-(3-methoxyphenyl)-N,N-dimethyl-N&#x2014;((S)-1-phenylethyl)ethanaminium, (S)-1-(3-hydroxyphenyl)-N,N-dimethyl-N&#x2014;((S)-1-phenylethyl)ethanaminium and (S)-1-(3-(ethyl(methyl)carbamoyloxy)phenyl)-N,N-dimethyl-N&#x2014;((S)-1-phenylethyl)ethanaminium, as well as a method for using (S)-1-(3-(ethyl(methyl)carbamoyloxy)phenyl)-N,N-dimethyl-N&#x2014;((S)-1-phenylethyl)ethanaminium to prepare rivastigmine which can be used for the treatment of Alzheimer's disease.

Preparation method for rivastigmine, intermediates thereof, and preparation method for said intermediates

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

Chunbo Yang