Synthesis and Selective N,O‐Functionalization of Pyrazolone‐Fused 3‐Aminoazepinones

Abstract

A new class of pyrazolone-fused 3-amino-1,3,4,7-tetrahydro-2H-azepin-2-ones was synthesized from azepane-based α,βunsaturated esters. The latter compounds were obtained efficiently from 2-Cbz-amino-N-(2-bromoallyl)-4-pentenamide derivatives through initial Pd-catalyzed methoxycarbonylation followed by ring-closing metathesis. These new 3- [a] Research