化学
酰胺
电泳剂
亲核细胞
药效团
组合化学
表面改性
烷基
催化作用
有机化学
立体化学
物理化学
作者
Matthieu Jouffroy,Jongrock Kong
标识
DOI:10.1002/chem.201806159
摘要
Abstract Nucleophilic radical additions at innately electrophilic C(sp 2 ) centers are perfectly suited for the direct functionalization of heterocycles. Using bench stable and commercially available alkyl oxamate and oxamic acid derivatives in combination with photoredox catalysis, a direct carbamoylation of heterocycles yielding amide functionalized pharmacophores in a single step is reported. The reaction conditions reported are compatible with structurally complex heterocyclic substrates of pharmaceutical interest. Notably, derivatives containing functional groups incompatible with standard amidation reactions, such as carboxylic acids and unprotected amines, were found to be amenable to this reaction paradigm.
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