化学
磺酰
有机化学
组合化学
反应条件
位阻效应
过渡金属
催化作用
烷基
作者
Qi Chen,Huanqing Li,Kai Yang,Wenjin Xu,Yu Zeng,Zhao‐Yang Wang
标识
DOI:10.1002/ajoc.202300418
摘要
Abstract An eco‐friendly and efficient synthesis of pyridazin‐3(2 H )‐ones from aromatic sulfonyl hydrazides and mucohalic acids has been developed. This facile strategy is carried out smoothly via the promotion of simple organic acid p ‐toluenesulfonic acid, and able to form two C−N bonds and a heterocycle linking a potentially bioactive sulfonyl group at one‐step. The protocol is tolerant to various readily available substrates in good yields, and pyridazin‐3(2 H )‐ones as the desired products are key structural fragments of many bioactive compounds. More importantly, the gram‐scale cyclization reaction of aromatic sulfonyl hydrazides and mucohalic acids as a novel approach to pyridazin‐3(2 H )‐ones derivatives successfully reveals its practicability.
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