Niu Huiying, Lu Lijun, Shi Renyi, Chiang Chien-Wei, Lei Aiwen
College of Chemistry and Molecular Sciences, Institute for Advanced Studies (IAS), Wuhan University, Wuhan 430072, P. R. China.
Chem Commun (Camb). 2017 Jan 17;53(6):1148-1151. doi: 10.1039/c6cc09072a.
Recently, utilizing CO as a methylation reagent to construct functional chemicals has attracted significant attention. However, the conversion of CO is still a challenge due to its inherent inertness. In this study, we have developed a catalyst-free N-methylation of amines to prepare numerous methylamines using CO as a methyl source. By utilizing 2 eq. PhSiH as the reductant, amines could undergo N-methylation under 1 atm of CO in DMF at 90 °C. Aliphatic and aromatic amines were compatible, generating the desired products in up to 95% yield.
最近，利用一氧化碳作为甲基化试剂来构建功能化学品引起了广泛关注。然而，由于一氧化碳本身的惰性，其转化仍然是一个挑战。在本研究中，我们开发了一种无催化剂的胺N-甲基化反应，以一氧化碳作为甲基源制备多种甲胺。通过使用2当量的苯基硅烷作为还原剂，胺可以在90℃、1个大气压的一氧化碳氛围下于N,N-二甲基甲酰胺中发生N-甲基化反应。脂肪族胺和芳香族胺均适用，目标产物的产率高达95%。
