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通过二氟乙酰腙酰溴与2-酰基乙腈或丙二腈环化合成全取代二氟甲基吡唑。

Synthesis of Fully Substituted Difluoromethylpyrazoles by Cyclization of Difluoroacetohydrazonoyl Bromides with 2-Acylacetonitriles or Malononitrile.

作者信息

Wang Si-Wei, Zhang Jianzhong, Deng Zhoubin, Lv Yuyu, Huang Danfeng, Wang Ke-Hu, Wang JunJiao, Hu Yulai

机构信息

College of Chemistry and Chemical Engineering, Northwest Normal University, Lanzhou 730070, PR China.

State Key Laboratory of Applied Organic Chemistry, Lanzhou University, Lanzhou 730000, PR China.

出版信息

J Org Chem. 2024 Aug 2;89(15):10591-10602. doi: 10.1021/acs.joc.4c00828. Epub 2024 Jul 12.

Abstract

A concise and efficient method for the construction of fully substituted difluoromethylpyrazoles is achieved by a cyclization reaction between difluoroacetohydrazonoyl bromides and 2-acylacetonitrile or malononitrile. The method features advantages such as mild reaction conditions, broad substrate scope, good product yields, and high regioselectivity.

摘要

通过二氟乙酰腙酰溴与2-酰基乙腈或丙二腈之间的环化反应,实现了一种简洁高效的构建全取代二氟甲基吡唑的方法。该方法具有反应条件温和、底物范围广、产物收率高和区域选择性高的优点。

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