Synthesis of 2-amino-9-chromeno[2,3-]thiazol-9-ones with anti-inflammatory activity cascade reactions of 2-amino-3 iodochromones with amines and carbon disulfide

A simple and efficient synthetic approach to 2-amino-9 H -chromeno[2,3- d ]thiazol-9-ones via copper-promoted cascade reactions was developed. The reaction employed easily available 2-amino-3-iodochromones and amines as substrates and the targeting tricyclic compounds could be obtained with moderate to good yields. Even more important, several synthesized compounds exhibited potent anti-inflammatory activities, which suggested that this protocol may provide valuable hits for drug development in the future. A concise and efficient protocol for constructing a chromone fused thiazole scaffold via a copper-promoted cascade reaction was developed. Representative compound c12 showed good anti-inflammatory activity.