Synthesis of withasomnine and pyrazole derivatives via intramolecular dehydrogenative cyclization, as well as biological evaluation of withasomnine-based scaffolds

文献情報

出版日 2017-11-29

DOI 10.1039/C7QO00847C

インパクトファクター 5.281

著者

Tingting Xia, Zhenyi Hu, Wenzhi Ji, Shujie Zhang, Hui Shi, Chenguang Liu, Bo Pang, Guijian Liu, Xuebin Liao

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要旨

Fragment-based drug discovery has recently drawn great attention from both industry and academia. Fragment library design is critical to success in this field. Herein we report our facile access to pyrazole derivatives via a cascade reaction involving a double C(sp3)–H functionalization and dehydrogenative aromatization sequence. Based on the newly developed method, we completed the synthesis of the Indian herbal medicine, withasomnine, in only two steps. In addition, inspired by the different biological activities of withasomnine, this cascade reaction sequence enables us to quickly build up a natural product-based fragment library. The compounds in this fragment library exhibit a variety of biological activities and demonstrate high hit rates on initial biological screening against COX-2.

掲載誌

Organic Chemistry Frontiers

CiteScore: 7.8

自己引用率: 8.7%

年間論文数: 724

Organic Chemistry Frontiers publishes high-quality research from across organic chemistry. Emphases are placed on studies that make significant contributions to the field of organic chemistry by reporting either new or significantly improved protocols or methodologies. Topics include, but are not limited to the following: Organic synthesis Development of synthetic methodologies Catalysis Natural products Functional organic materials Supramolecular and macromolecular chemistry Physical and computational organic chemistry

Synthesis of withasomnine and pyrazole derivatives via intramolecular dehydrogenative cyclization, as well as biological evaluation of withasomnine-based scaffolds

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