Zhejiang Hisun Pharmaceutical Co., Ltd.

Shanghai Institute of Pharmaceutical Industry

Pengcheng Qiu

Fuli Zhang

Jian Chai

Qingfeng Cai

Jiang Li

Bin Liang

Zhezhou Yang

Rusheng Bao

Weiwei Xu

Hairong Luo

Chunbo Yang

Chonghao Liu

Linyong Jin

Hu Pan

Linyu Pan

Dongming 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

The present invention provides a key new intermediate (a compound of formula III) of 4-benzyl-1-phenethyl-piperazine-2,6-dione (formula IV compound), a pharmaceutically acceptable salt thereof and a preparation method thereof. The present invention additionally discloses a method for preparing 4-benzyl-1-phenethyl-piperazine-2,6-dione (formula IV compound) from the formula III compound, said method overcoming the shortcomings of current formula IV compound preparation methods, such as low production volumes, low purity, high energy consumption, high costs, and inability to achieve industrialized production, and provides a formula IV compound preparation method which is simple, economical, environmentally-friendly and easy to produce industrially; the reaction solvent of the method is easily recycled and the method can produce the formula IV compound at high production rates and with high purity. 

4-benzyl-1-phenethyl-piperazine-2,6-dione preparation method, and intermediate and preparation method thereof

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

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Shanghai, China

Pengcheng Qiu