Zhejiang Hisun Pharmaceutical Co., Ltd.

Qifeng Zhu

Hua Bai

Xuyang Zhao

Xiaoyu Liu

Xiaojie Xu

Yuncai Zhang

Yong Zhang

Yongxiang Gong

Jinqing Zhong

Jian Zhang

Zhiqing Yang

Xiaohe Zheng

Dezhou Xu

Li Zhang

Xiaoming Wang

Zehua Zhong

Lifei Liu

Xufei Li

Maojian Gu

Hairong Luo

Xinlong Zhang

Weiwei Liu

Qixian Zhou

Ya Zhou

Ying Chen

Disclosed are a method for preparing a benzodioxole derivative (AD-35) shown by Formula (I) and an intermediate thereof. The method of the present invention involves: using piperic acid as a raw material; and performing bromination, esterification, cyanidation, cyclopropane lactamization, amide nitrogen alkylation, deprotection, piperidine nitrogen alkylation and salification to obtain the compound of Formula (I). The method has cheap and easily available start raw materials, short synthesis routes and simple operation, and is suitable for industrial production. 

Process for preparing AD-35

Disclosed is a new method for preparing an azetidinone compound represented by formula (I). The carboxylic ketoester represented by formula (II) serves as the raw material and is subjected to Grignard addition, stereoselective dehydration, ester group reduction, hydroxyl group protection, addition with imine after condensation with a chiral auxiliary, cyclization and deprotection to obtain the compound represented by formula (I). The present invention has advantages of easily available raw material, a few synthetic steps, simple operation, high yield, good stereoselectivity and low cost, and can be used for industrial production. 

Method for preparing azetidinone compound and intermediate of azetidinone compound

Provided in the present invention are novel benzodioxole derivatives and preparation methods thereof. These compounds represented by formula (I) or pharmaceutically acceptable salts thereof have acetylcholinesterase inhibitory activity, so can be used in the treatment or prevention of Alzheimer's disease. The definitions of R, Rand A of formula (I) can be seen in the description. 

Benzodioxole derivative and preparation method and use thereof

Provided are a benzamide derivative as shown in formula (I) or a pharmaceutically acceptable salt thereof, and the preparation method and use thereof for preparing a medicine for treating cancer, wherein the group definitions of formula (I) are as set out in the description. 

Benzamide derivative with anticancer activity and preparation method and use thereof

Preparation of azetidinone compounds and medical use thereof are provided by the present invention. More particularly, azetidionne compounds, shown as formula (I), wherein R, R, R, R, Rand Rare defined in description, and preparation methods thereof are provided by the present invention. The compounds of the present invention can reduce the levels of total cholesterol (TC) and low density lipoprotein cholesterol (LDL-C) in plasma, and can be used as medicaments for reducing cholesterol in blood. Therefore the compounds of the present invention can be used to treat or prevent diseases of atherosclerosis, cacergasia of blood vessel, cardiac failure, coronary artery disease, angiocardiopathy, myocardial, angina, hyperlipoidemia and hypercholesteremia and the like. Preparation method of compounds of formula (I) and intermediate compounds are also provided by the present invention. 

Azetidinone compounds and medical use thereof

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Taizhou, China

Qifeng Zhu