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Rh(III)-catalyzed C–H acylmethylation of 2H-indazoles with sulfoxonium ylides
Journal of Saudi Chemical Society ( IF 5.8 ) Pub Date : 2020-09-20 , DOI: 10.1016/j.jscs.2020.09.001
Ya-Gai Wang , Jing Li , Xiao-Die Wang , Linlin Shi , Xinju Zhu , Xin-Qi Hao , Mao-Ping Song

An efficient Cp*Rh(III)-catalyzed direct acylmethylation of 2H-indazoles with sulfoxonium ylides has been realized under air atmosphere via chelation-assisted strategy. This protocol enables a regioselective access to a variety of ortho-acylmethylated 2-phenylindazole derivatives in moderate to good yield, which has the advantages of broad substrate scope, good functional group tolerance, and operational convenience. The H/D exchange experiment reveals that a reversible cleavage of C–H bond might not be the rate-limiting step in this transformation.



中文翻译:

Rh(III)催化2 H-吲唑与亚砜基鎓盐的C–H酰基甲基化

通过螯合辅助策略,在空气中实现了高效的Cp * Rh(III)催化2 H-吲唑与亚砜基鎓的直接酰基甲基化反应。该方案使得能够以中等至良好的收率选择性地选择各种邻-酰基甲基化的2-苯基吲唑衍生物,其优点是底物范围宽,官能团耐受性好和操作方便。H / D交换实验表明,C–H键的可逆裂解可能不是此转化过程中的限速步骤。

更新日期:2020-10-30
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