摘要

A new efficient synthesis of 6, 12-dihydro-5H-quinazolino[3,2-a]quinazolin-5-ones by sequential Ugi/Staudinger/aza-Wittig/addition/nucleophilic acyl substitution has been developed. alpha-Amino amides, obtained from Ugi-3CR of 2-azidobenzaldehydes, methyl 2-aminobenzoates, and isocyanides in the presence of catalytic amount of phenylphosphinic acid, reacted with triphenylphosphine and isocyanates to give 6, 12-dihydro-5H-quinazolino[3,2-a]quinazolin-5-ones in good yields. This method provides a domino and effective strategy for the preparation of various substituted quinazolino[3,2-a]quinazolin-5-ones under mild reaction condition.