Synthesis 2024; 56(09): 1449-1459
DOI: 10.1055/a-2241-6697
paper

Metal-Free N-Formylation of Amines Using Carbohydrates as C1 Synthon via C–C Bond Cleavage

Shital Atpadkar
,

The study was supported by National Institute of Pharmaceutical Education & Research S.A.S. Nagar Punjab (India).


Abstract

Formamide group is an important part of many drug molecules, and herein a process for N-formylation of amines using carbohydrates as the C1 synthon under oxidative metal-free reaction conditions has been reported for the first time. Literature syntheses of formamides uses toxic, moisture sensitive and costly reagents under harsh reaction conditions. Our metal-free formylation is a facile, economical, and an efficient process of broad substrate scope that has led to the synthesis of thirty-three N-formylated compounds in excellent isolated yields.

Supporting Information



Publication History

Received: 31 October 2023

Accepted after revision: 10 January 2024

Accepted Manuscript online:
10 January 2024

Article published online:
07 February 2024

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