文献类型：期刊文献

英文题名：A One-pot Approach to Ethyl 1,4,5-Triaryl-1H-pyrazole-3-carboxylates via an Improved Claisen Condensation-Knorr Reaction Sequence

作者：Zhai, Jiaojiao[1];Gu, Chunhui[1];Jiang, Jianan[1];Zhang, Shunli[1];Liao, Daohua[1];Wang, Lei[2];Zhu, Dunru[2];Ji, Yafei[1]

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

年份：2013

卷号：31

期号：12

起止页码：1526

外文期刊名：CHINESE JOURNAL OF CHEMISTRY

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000329998100009)，CCR-EXPANDED(收录号:WOS:000329998100009)】；

基金：The authors are grateful to the National Natural Science Foundation of China (Nos. 21176074 and 21171093) for financial support.

语种：英文

外文关键词：one-pot approach; 2; 4-dioxo-3; 4-diarylbutanoates; Claisen condensation; Knorr reaction; triarylpyrazole-3-carboxylates

摘要：A one-pot approach to ethyl 1,4,5-triaryl-1H-pyrazole-3-carboxylates has been developed in moderate to high yields. The tert-BuOLi-mediated Claisen condensation of 1,2-diarylethanones and ethyl oxalyl chloride efficiently provided the enolized lithium salts of ethyl 2,4-dioxo-3,4-diarylbutanoates, which in situ reacted with arylhydrazine hydrochlorides via a hydrochloric acid-promoted Knorr reaction to produce the exquisite triarylpyrazole-3-carboxylates. The procedure promises a convenient access to this highly crowded framework for drug discovery.