Chinese Academy of Sciences

Shuni Wang

Hong Tao Liu

Jiang Wang

Hualiang Jiang

Kaixian Chen

Wei Zhu

Jun Wei Zhang

Jia Tao Li

Yubo Zhou

Mingbo Su

Chunpu Li

Hong Liu

Weijuan Kan

Shengbin Zhou

Panfeng Peng

Hao Shen

Yong Nian

Shuangjie Shu

Wei Xu

Jia Li

The present invention relates to the fields of medicinal chemistry and pharmacotherapy, and specifically relates to the chemical compound of formula (I), and its racemate, R-isomer, S-isomer, pharmaceutically acceptable salt, and mixtures thereof, as well as its method for preparation, a pharmaceutical composition containing said chemical compound, and use as a lysine-specific demethylase 1 (LSD 1) inhibitor. The cyclopropylamine chemical compound to which the present invention relates may be used in the treatment of cancer.

Trans-indoline cyclopropylamine chemical compound, and method for preparation, pharmaceutical composition, and use thereof

Disclosed is a method for synthesizing a novel chiral ligand, a metal chelate, a variety of non-natural amino acids, Maraviroc and a key intermediate thereof. In the invention, (R)-2-methyl proline is selected and used as a starting raw material, (S)-&#x3b2;-amino acid is obtained by asymmetric resolution induced by using a nickel chelate, and Maraviroc is synthesized by using (S)-3-amino-3-phenylpropionic acid as a key intermediate with a high yield and the ee value reaching 98.2% or more. The method of the present invention has widely available materials, mild synthetic process conditions, is easy to control, and produces a product of a high optical purity.

Method for synthesizing novel chiral ligand, metal chelate, a variety of non-natural amino acids, maraviroc and key intermediate thereof

Provided is a fluorinated cyclopropylamine compound represented by formula I, a racemate thereof, an R-isomer thereof, an S-isomer thereof, a pharmaceutical salt thereof, and a mixture thereof. Also provided are pharmaceutical compositions containing the compound, a preparation method for the compound, and uses thereof as a lysine specific demethylase 1 (LSD1) inhibitor, and in the treatment of cancers. 

Fluorinated cyclopropylamine compound, preparation method therefor, pharmaceutical composition thereof, and uses thereof

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Shanghai, China

Shuni Wang