Department of Chemistry, Visva-Bharati (A Central University) , Santiniketan 731235, India.
Org Lett. 2017 Jul 21;19(14):3751-3754. doi: 10.1021/acs.orglett.7b01594. Epub 2017 Jul 5.
A hitherto unreported aminomethylation occurs at C-3 of imidazopyridines with morpholine in the presence of (diacetoxyiodo)benzene at ambient temperature in short reaction times. This methodology is also applicable to indolizine, imidazo[2,1-b]thiazole, benzo[d]imidazo[2,1-b]thiazole, and indole. Interestingly, the aminomethylation involving morpholine as a source of methylene group is a new phenomenon. This protocol is of much potential for the synthesis of aminomethylated derivatives under mild reaction conditions.
在环境温度下，用（二醋酸碘苯）作为氧化剂，在短时间内，3-位的咪唑并吡啶与吗啉发生氨基甲基化反应，这是一个以前未曾报道过的反应。该方法也适用于吲哚嗪、咪唑并[2,1-b]噻唑、苯并[d]咪唑并[2,1-b]噻唑和吲哚。有趣的是，吗啉作为亚甲基来源的氨基甲基化是一个新现象。该方法在温和的反应条件下，为合成氨基甲基化衍生物提供了很大的潜力。
