Solvent-free Zinc-catalyzed Amine N-Formylation

摘要

Formamides are important intermediates in the preparation of amine derivatives and have been widely used in the synthesis of pharmaceutically valuable compounds. They have also been employed as reagents in Vilsmeier formylation and in the allyl-ation and hydrosilylation ofcarbonyl compounds. In addition, the formyl group is an important amine-protecting group in peptide synthesis. Various reagents for the synthesis of form-amides have been developed including formic acid with activating reagents such as DCC, EDCI, CDMT, PEG-400, or Lewis acids, formic acid derivatives such as acetic formic anhydride, 2,2,2,-trifluoroethyl formate and pentafluoro-phenyl formate, cyanomethyl formate, ammonium formate, and solid-supported reagents. However, these agents are moisture sensitive, highly toxic, and expensive.