A novel method for the synthesis of nicotinonitrile and diazepin derivatives under microwave irradiation

الملخص EN

Ethyl 2-aryl-3-dimethylamino-acrylates 2a, b were prepared via the reaction of ethyl ary-lacetate with JV, Af-dimethylformamidedimethylacetal (DMFDMA) under microwave irradiation.

Reaction of 2a, b with malononitrile afforded the corresponding substituted malononitrile derivatives 4a, b, which underwent intermolecular cyclization in boiling acetic acid, containing a catalytic amount of ammonium acetate, to give unexpected products 2-amino-6-hydroxy-5-(4-nitro-phenyl) nicotinonitrile derivatives 6.

Whereas 2a reacted with o-phenylenediamines under microwave irradiation to yield diazepin-4-ol derivative 9.

On the other hand, reacting the enaminoesters 2a, b with urea and thiourea, as nitrogen nucleophiles, by heating under microwave yielded the pyrimid-inone derivatives 12a-d.