Zhejiang Hisun Pharmaceutical Co., Ltd.

Shanghai Institute of Pharmaceutical Industry

China National Medicines Guorui Pharmaceutical Co., Ltd.

Chonghao Liu

Fuli Zhang

Yang Gao

Jian Chai

Bin Liang

Jian Wang

Qingfeng Cai

Pengcheng Qiu

Chunbo Yang

Min Jiang

A molecule with neural activities, especially 4-substituent-2-hydroxymorpholin-3-one, as a new intermediate of neurokinin-1 receptor antagonist aprepitant, and preparation method thereof. 

4-substituent-2-hydroxylmorpholine-3-one and preparation method thereof

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

Chonghao Liu