文献类型：期刊文献

英文题名：One-Pot Synthesis of Highly Substituted 1H-Pyrazole-5-carboxylates from 4-Aryl-2,4-diketoesters and Arylhydrazines

作者：Zhai, Jiao-Jiao[1];Gu, Chun-Hui[1];Guo, Ying[1];Liao, Dao-Hua[1];Zhu, Dun-Ru[2];Ji, Ya-Fei[1]

机构：[1]E China Univ Sci & Technol, Sch Pharm, Campus POB 363,130 Meilong Rd, Shanghai 200237, Peoples R China;[2]Nanjing Tech Univ, Coll Chem & Chem Engn, State Key Lab Mat Oriented Chem Engn, Nanjing 210009, Jiangsu, Peoples R China

年份：2016

卷号：53

期号：3

起止页码：840

外文期刊名：JOURNAL OF HETEROCYCLIC CHEMISTRY

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000374982900022)，CCR-EXPANDED(收录号:WOS:000374982900022)】；

基金：The authors are grateful to the National Natural Science Foundation of China (Project Nos. 21176074, 21476074, 21476115 and 21171093) and Research Fund for the Doctoral Program of Higher Education of China (Project No. 20130074110009) for financial support.

语种：英文

摘要：A one-pot synthesis of highly substituted 1H-pyrazole-5-carboxylates 1 has been developed starting from easily available 4-aryl-2,4-diketoesters 2 and arylhydrazine hydrochlorides 3. More active 2-carbonyl group of 2 was blocked with methoxyamine hydrochloride to give 2-methoxy imine intermediates, which were then subjected to condensation cyclization with 3 in situ to provide the desired products 1. In addition, the geometrical configuration of 1aa was unambiguously confirmed by single crystal X-ray crystallography.