Facile synthesis of (β-chlorodifluoroethyl)phosphonates via chlorination reaction of difluoroalkyl diazo derivatives with HCl
Facile synthesis of (β-chlorodifluoroethyl)phosphonates via chlorination reaction of difluoroalkyl diazo derivatives with HCl
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DOI：
10.1016/j.cclet.2021.10.066
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发表时间：
2022-04-27
影响因子：
9.1
通讯作者：
Han, Jianlin
中科院分区：
文献类型：
--
作者：
Liu, Jiang;Pajkert, Romana;Han, Jianlin
以盐酸为氯源，在温和且操作方便的条件下，实现了原位生成的(β-重氮-α,α-二氟乙基)膦酸酯的高效氯化反应。该反应不需要任何催化剂，并且能耐受多种底物，从而以良好至优异的产率提供（β-氯二氟乙基）膦酸酯产品。该反应代表了二氟烷基重氮化合物卤化的第一个例子，也为合成含二氟亚甲基膦酸酯的化合物提供了一种简单的方法。 (C) 2021 由Elsevier B.V.代表中国化学会和中国医学科学院药物研究所出版。
An efficient chlorination reaction of in situ generated (beta-diazo-alpha,alpha-difluoroethyl)phosphonates has been achieved with hydrochloric acid as a chlorine source under mild and operationally convenient conditions. The reaction does not need any catalyst and tolerates a wide scope of substrates, which affords the (beta-chlorodifluoroethyl)phosphonate products in good to excellent yields. This reaction represents the first example of the halogenation of difluoroalkyl diazo compounds, and also provides an easy way for the synthesis of difluoromethylenephosphonate-containing compounds. (C) 2021 Published by Elsevier B.V. on behalf of Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences.