Chinese Academy of Sciences

Topharman Shanghai Co., Ltd.

Topharman Shandong Co., Ltd.

Xianguo Zhao

Xiangrui Jiang

Zheng Liu

Hualiang Jiang

Zhen Wang

Jingshan Shen

Guan Zhong Wang

Jianfeng Li

Guanghui Tian

Xiaojun Yang

Rongxia Zhang

Weiming Chen

Fuqiang Zhu

Jin Suo

Weiliang Zhu

Xudong Gong

Zhu Xie

The present invention relates to new salts of pyrazolopyrimidinone represented by formula (I), and pharmaceutically acceptable polymorph, solvate, hydrate, dehydrate, co-crystallization, anhydrous, or amorphous form thereof, the pharmaceutical compositions, and a pharmaceutical unit dosage form containing the same, wherein x represents organic or inorganic acids, preferable maleic acid, succinic acid, methanesulfonic acid, hydrochloric acid, etc. The invention further relates to co-crystals or complexes of compounds of pyrazolopyrimidinone and pharmaceutical compositions containing the same. The present invention also relates to a process for the preparation, use thereof and pharmaceutical preparation containing the salts or crystalline forms. 

Salt and polymorph of pyrazolopyrimidinone compound, and pharmaceutical composition containing the same, preparation method and use thereof

This invention disclose (2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone in a single configuration and preparation method and use thereof. The (2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone, or a pharmaceutically acceptable salt, an ester, a prodrug or a solvate thereof according to the invention are important intermediates of a variety of anti-viral and anti-tumor active ingredients. A compound obtained from (2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone via an acylation reaction can be directly used for preparing various anti-viral and anti-tumor drugs. The Chiral synthesis method and the spontaneous resolution method of the compound of (2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone according to the invention have the following advantages: the reaction routes are short and simple with high yield and low cost, which are suitable for industrial application. 

(2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone and preparation method and use thereof

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Shanghai, China

Xianguo Zhao