Efficient solid-phase synthesis of a library of imidazo1,2-apyridine-8-carboxamides

摘要

A versatile method for the solid-phase synthesis of imidazo1,2-apyridine-based derivatives, imidazo1,2-apyridine-8-carboxamides, has been developed. They were obtained by treatment of the amino group of the polymer-bound 2-aminonicotinate with different alpha-haloketones, followed by halogenation at the 3-position of the polymer-bound imidazo1,2-apyridine. The derived polymer-bound imidazo1,2-apyridines 5, 6, and 7 were finally cleaved from the solid-support with an excess of primary or secondary amines. The final crude products were purified from excess amines by solid-supported liquid-liquid extraction (SLE).