Department of Chemistry, National Chung Hsing University, Taichung, 402, Taiwan.
Org Biomol Chem. 2020 Aug 7;18(29):5726-5733. doi: 10.1039/d0ob01080d. Epub 2020 Jul 15.
N-Formamide synthesis using N-formyl imide with primary and secondary amines with catalytic amounts of p-toluenesulfonic acid monohydrate (TsOH·HO) is described. This reaction is performed in water without the use of surfactants. Moreover, N-formyl imide is efficiently synthesized using acylamidines with TsOH·HO in water. In addition, N-formyl imide was successfully used as a carbonyl source in the synthesis of benzimidazole and quinazolinone derivatives. Notable features of N-formylation of amines by using N-formyl imide include operational simplicity, oxidant- and metal-free conditions, structurally diverse products, and easy applicability to gram-scale operation.
使用一水对甲苯磺酸（TsOH·HO）催化量的 N-甲酰亚胺与伯胺和仲胺合成 N-甲酰胺的方法。该反应在水中进行，无需使用表面活性剂。此外，使用 TsOH·HO 可以有效地在水中合成 N-甲酰亚胺。此外，N-甲酰亚胺还成功地用作合成苯并咪唑和喹唑啉酮衍生物的羰基源。使用 N-甲酰亚胺甲酰化胺的显著特点包括操作简单、无氧化剂和金属条件、结构多样的产物以及易于适用于克级规模操作。
