Chinese Academy of Sciences

Topharman Shanghai Co., Ltd.

Kai Xie

Zheng Liu

Jingshan Shen

Jing Shi

Jianfeng Li

Ye Li

Jin Zheng

Haihong Li

Yongjun Mao

The present invention relates to a method for preparing 6-substituted amino-3-cyanoquinoline compounds (compound A for short) and the intermediates thereof, more particularly, to a compound of the following formula (I), the preparation method thereof, the intermediates thereof and use thereof for preparing the compound A. The compound of the formula (I) is cyclized in the presence of an alkali to give a compound of formula A, wherein W is OH; or the compound of the formula (I) is cyclized in the presence of an alkali, and then chlorinated to give a compound of the formula A, wherein W is Cl. Compared with the known methods in the literature, the method for preparing the compound A from the compound of formula (I) according to the present invention can avoid using high-temperature condition and high boiling point solvents, and is safe and environment-friendly, mild in reaction condition, easy in operation with a high yield and high product purity. 

Preparation methods of 6 substituted amino-3 cyanoquinoline compounds and the intermediates thereof

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Shanghai, China

Kai Xie