Abstract
The carbodiimides 2, obtained from aza-Wittig reactions of iminophosphorane 1 with aromatic isocyanates, reacted with ammonia to give ethyl 3,4-dihydro-6-methyl-4-oxo-2-arylamino-furo[2,3- d]pyrimidine-5-carboxylate 3. Further reaction of 3 with POCl 3 and various amines generated ethyl 4-alkylamino-2-arylamino-6-methyl-furo[2,3- d]pyrimidine-5-carboxylate 5 in good yields. Their structures were confirmed by 1H NMR, EI-Ms, IR and elemental analysis. Compound 5b was further analyzed by single crystal X-ray diffraction. Compound 5 exhibited cytotoxicity against two lung cancer cell lines. For example, compound 5a showed the best inhibition activities against A459 with IC 50 0.8 μM.
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