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Multicomponent Cyclization with an Inorganic Sulfur Dioxide Surrogate: Straightforward Construction of Difluorinated Benzosultams
Organic Letters ( IF 4.9 ) Pub Date : 2022-12-01 , DOI: 10.1021/acs.orglett.2c03771
Yu-Heng Wu 1 , Cheng-Jing Li 1 , Zhong-Lin Wei 1 , Wei-Wei Liao 1, 2
Affiliation  

A straightforward three-component transformation for the preparation of functionalized benzosultams under TM-free and mild reaction conditions was described, in which easy-to-handle Na2S2O5, available bromodifluoroalkyl reagent, and N-(2-haloaryl) cyanamide were employed. Na2S2O5 was essential to the generation of difluoroalkyl radical, SO2 fixation, and cyclization, which enabled efficient construction of target products in a sustainable manner. A broad substrate scope and modular feature made this protocol attractive for exploring the chemical space of the construction of cyclic sulfonamides.

中文翻译:

用无机二氧化硫替代物进行多组分环化:直接构建二氟化苯并磺胺

描述了在无 TM 和温和反应条件下用于制备官能化苯甲磺胺的直接三组分转化,其中易于处理的 Na 2 S 2 O 5、可用的溴二氟烷基试剂和N-(2-卤代芳基)氰胺被雇用。Na 2 S 2 O 5对于二氟烷基自由基的产生、SO 2固定和环化是必不可少的,这使得能够以可持续的方式高效构建目标产物。广泛的底物范围和模块化特征使该协议对于探索环状磺胺类化合物的化学空间具有吸引力。
更新日期:2022-12-01
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