二氟甲基重氮甲烷作为含氟砌块的应用研究进展  

Recent Progress in the Application of Difluoromethyl Diazomethane as Fluorine-Containing Building Block

作　　者：朱文庆[1] 许婷怡 韩文勇 Wenqing Zhu;Tingyi Xu;Wenyong Han(School of Environmental and Chemical Engineering,Xi'an Polytechnic University,Xi'an 710048;Key Laboratory of Biocatalysis&Chiral Drug Synthesis of Guizhou Province,School of Pharmacy,Zunyi Medical University,Zunyi,Guizhou 563006;Key Laboratory of Basic Pharmacology of Ministry of Education and Joint International Research Laboratory of Ethnomedicine of Ministry of Education,Zunyi Medical University,Zunyi,Guizhou 563006)

机构地区：[1]西安工程大学环境与化学工程学院,西安710048 [2]遵义医科大学药学院贵州省生物催化与手性药物合成重点实验室,贵州遵义563006 [3]遵义医科大学基础药理教育部重点实验室暨特色民族药教育部国际合作联合实验室,贵州遵义563006

出　　处：《有机化学》2021年第4期1275-1287,共13页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(No.21762054);遵义医科大学优秀青年人才支持计划(No.18ZY-002)资助项目。

摘　　要：二氟甲基化反应经过近二十年的发展已取得了较为显著的研究成果.除直接和间接二氟甲基化反应外,二氟甲基砌块参与的化学转化是一种向有机化合物中引入二氟甲基的新策略.相比于亲电、亲核和自由基二氟甲基化试剂,二氟甲基砌块的种类仍然有限并有待进一步开发.其中,二氟甲基重氮甲烷是近年来发展的一类新型含氟砌块,受到了研究学者们的高度关注.综述了二氟甲基重氮甲烷及其稳定替代物的最新应用研究进展,着重介绍了其反应类型及相关机理,并对今后的发展方向进行了展望.Difluoromethylation has achieved remarkable progress in the past two decades.In addition to the direct difluoromethylation and the stepwise difluoromethylation,chemical transformation starting from CF2H-containing building blocks is a novel strategy to introduce difluoromethyl group into organic compounds.Compared with electrophilic-,nucleo-philic-and free radical-difluoromethylation reagents,the types of CF_(2)H-containing building blocks are still limited and less explored.Among them,difluoromethyl diazomethane(CF_(2)HCHN_(2))is a new type of fluorine-containing building block developed in recent years,which has received much attention from researchers.The recent progress in the application of difluoromethyl diazomethane and its surrogates as fluorine-containing building blocks is summarized,focusing on the reaction types and related mechanisms,and the developmental direction in the future is prospected.

关 键 词：二氟甲基重氮甲烷 二氟甲基化 含氟砌块 吡唑 

分 类 号：O621.25[理学—有机化学]