Solvent-free microwave multicomponent regiospecific synthesis of pyrimido[4,5-c]isoquinolines and evaluation in vitro of their antifungal properties.

JAIRO QUIROGA; CISNEROS, C; BRAULIO INSUASTY; RODRIGO ABONIA; NOGUERAS MANUEL; SORTINO, MAXIMILIANO; ZACCHINO SUSANA

JOURNAL OF HETEROCYCLIC CHEMISTRY

Año: 2006 vol. 43 p. 463 - 469

0022-152X

The free-solvent multicomponent reaction under microwave irradiation of 6-aminopyrimidin-4(3H)-ones (1) with dimedone (2) and N,N-dimethylformamide dimethylacetal yields the pyrimido[4,5-c]isoquinolinones (5a-j). In this process, the intermediate of cyclization was isolated. The structure of the synthesized compounds was determined on the basis of nmr measurements, especially by 1H,1H-,1H,13C COSY, and DEPT. These compounds showed antifungal in vitro activity particularly against dermatophytes.