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.
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1,4-Dioxane-Tuned Catalyst-Free Methylation of Amines by CO and NaBH.
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MOE Key Laboratory of Bioorganic Phosphorus Chemistry & Chemical Biology, Department of Chemistry, Tsinghua University, Beijing, 100084, China.
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College of Chemistry and Molecular Sciences, Institute for Advanced Studies (IAS), Wuhan University, Wuhan 430072, P. R. China. and National Research Center for Carbohydrate Synthesis, Jiangxi Normal University, Nanchang 330022, P. R. China.
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.
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