Abstract Salicylaldehydes and protected 1, 2-amino alcohols have been convergently converted into a series of 2, 3-dihydrobenzo [f][1, 4] oxazepines, which undergo an Ugi– Joullié multicomponent reaction with unusual long-range diastereoselectivity. This protocol allows the diastereoselective preparation, in only two steps, of a series of drug-like tetrahydrobenzo [f][1, 4] oxazepines, with the combinatorial introduction of four diversity ...
