Rapid synthesis of 3-amino isocoumarin derivatives from ynamides

Abstract

A novel and efficient fast synthesis of 3-amino isocoumarins in good to excellent yields is reported. These interesting scaffolds can be obtained either in a single step from readily available ynamides or in a two-step sequence from the corresponding alkynyl bromide after C–N cross-coupling. This protocol, which only requires a Brønsted or Lewis acid as a promoter, offers an alternative approach toward synthesizing 3-substituted isocoumarins under smooth and fast conditions.