An efficient synthesis of spiro-pyrimidine derivatives from malononitrile, isatin and amidine

Pyrimidine derivatives occupy a unique place in medicinal chemistry because of their presence in several bioactive substances such as antibacterial, antiviral, and anti-HIV agents.1 Moreover, pyrimidine based spirocyclic systems have been of considerable interest due to their pronounced biological properties such as fredericamycine, acorenone, β-vetivone, and isocomene, which are isolated from plants.2 A useful and simple strategy for the synthesis of spiro-pyrimidines derivatives via a three-component reaction between isatin 1, malononitrile 2, and amidine 3, in the ethanol in the presence of 3 drop of Et3N as a basic catalyst under reflux conditions is described in this study (Fig. 1). All the synthesized compounds were unknown to the best of our knowledge and were characterized by 1H, 13C- NMR, and IR.

Keywords:

Malononitrile , Isatin , Amidine , Spiro-pyrimidines derivatives