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2,2-Difluoroethylation of Heteroatom Nucleophiles via a Hypervalent Iodine Strategy
Angewandte Chemie International Edition ( IF 16.1 ) Pub Date : 2024-06-20 , DOI: 10.1002/anie.202410954
Suman Das 1 , Charlotte McIvor 1 , Andrew Greener 1 , Charlotte Suwita 1 , Stephen P Argent 1 , Miriam L O'Duill 1
Affiliation  

A new hypervalent iodine(III) reagent is disclosed for 2,2-difluoroethylation of thiols, amines and alcohols via a proposed ligand coupling mechanism. A range of pharmaceutically relevant nucleophiles are difluoroethylated, including morpholine, glucose and the drugs Captopril, Normorphine and Mefloquine.

中文翻译:


通过高价碘策略对杂原子亲核试剂进行 2,2-二氟乙基化



公开了一种新的高价碘 (III) 试剂,用于通过拟议的配体偶联机制对硫醇、胺和醇进行 2,2-二氟乙基化。一系列与药学相关的亲核试剂被二氟乙基化,包括吗啉、葡萄糖和药物卡托普利、去甲吗啡和甲氟喹。
更新日期:2024-06-20
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