Zhejiang Hisun Pharmaceutical Co., Ltd.

Shanghai Institute of Pharmaceutical Industry

Daoxin Chen

Hua Bai

Fuli Zhang

Rentong Sun

Zhiqing Yang

Zhezhou Yang

Rusheng Bao

Meihua Xie

Chunbo Yang

Meng Hu

Anping Lai

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

The present invention provides N-methylethylcarbamino-3-[(S)-1-(methyl-[(S)-1-phenylethyl]amino)ethyl]phenyl ester represented by formula (II) and its preparation method. The present invention also provides (S)-1-(3-methoxyphenyl)-N-methyl-N&#x2014;[(S)-1-phenylethyl]ethylamine and 3-[(S)-1-(methyl-[(S)-1-phenylethyl]amino)ethyl]phenol as intermediates of the compound represented by formula (II), and the use of the compound represented by formula (II) for preparing rivastigmine used for treating Alzheimer disease.

Preparation method of rivastigmine, its intermediates and preparation method of the intermediates

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Zhejiang, China

Daoxin Chen