One-Pot Reductive Am ination/N-Acylation/Aza-Wittig Reaction for the Synthesis of 3,4-Dihydroquinazolines
A one-pot three-step synthesis for the preparation of 3,4-dihydroquinazolines is developed.This method involves a reductive amination of o-azidebenzaldehydes with amines followed by N-acylation using azoyl chloride and Staudinger/intramolecular aza-Wittig sequence in the presence of P(Bu-n)3.Aromatic amines,benzylamines,and aliphatic chain amines could complete this multi-step reaction.The yield of butylamine,however,was slightly lower.Satisfactory yields can be ob-tained when aromatic acyl chloride containing electron-donating groups on the benzene ring was used.However,aromatic acyl chloride with electron withdrawing chlorine atoms and acryloyl chloride failed to give the corresponding products.
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