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铜催化的4-三氟甲基吡唑的化学选择性合成

Copper-catalyzed chemoselective synthesis of 4-trifluoromethyl pyrazoles.

作者信息

Lu Jiaqing, Man Yuning, Zhang Yabin, Lin Bo, Lin Qi, Weng Zhiqiang

机构信息

Fujian Provincial Key Laboratory of Electrochemical Energy Storage Materials, College of Chemistry, Fuzhou University Fuzhou 350108 China

Ocean College, Minjiang University Fuzhou 350108 China

出版信息

RSC Adv. 2019 Sep 30;9(53):30952-30956. doi: 10.1039/c9ra07694h. eCollection 2019 Sep 26.

Abstract

A series of 4-trifluoromethyl pyrazoles have been prepared the copper-catalyzed cycloaddition of 2-bromo-3,3,3-trifluoropropene with a variety of -arylsydnone derivatives under mild conditions. This new protocol under optimized reaction conditions [Cu(OTf)/phen, DBU, CHCN, 35 °C] afforded 4-trifluoromethyl pyrazoles in moderate to excellent yields with excellent regioselectivity.

摘要

通过在温和条件下,使2-溴-3,3,3-三氟丙烯与多种芳基斯德酮衍生物进行铜催化的环加成反应,制备了一系列4-三氟甲基吡唑。在优化的反应条件[Cu(OTf)/邻菲罗啉、DBU、乙腈、35℃]下,这一新方法以中等至优异的产率和优异的区域选择性得到了4-三氟甲基吡唑。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1478/9072218/5881de1486b0/c9ra07694h-f1.jpg

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