A new facile synthesis of 3,4-dihydroquinazoline-2(1 H)-thiones by an Ugi-azide/Staudinger/aza-Wittig/cyclization sequence has been developed. The Ugi-azide reactions of 2-azidobenzaldehydes, amines, trimethylsilyl azide, and isocyanides produced tetrazoles, which, when treated with methyldiphenylphosphane and CS 2, produced 3,4-dihydroquinazoline-2(1 H)-thiones in good overall yields via a sequential Staudinger/aza-Wittig/cyclization reac...