SYNTHESIS OF SOME 4(3H)-PYRIMIDINONE DERIVATIVES OF POTENTIAL ANTIVIRAL ACTIVITY

Abstract

The thesis is prefaced by a survey on the biologically active 2-amino-4(3H)-pyrimidinone derivatives.

In the course of a current program directed at this laboratory towards the design and synthesis of novel antivi­ ral and antineoplastic compounds, the presented thesis con­ tains the synthesis and preliminary cytotoxic and antiviral investigations of certain 2-amino-5,6-disubstituted-4(JH)­ pyrimidinones The rationale for the design of such compounds stems from the suggestion that such structures simulate that of the interferon inducing agent, bropirimine (LXVI, R= C6H5, R1= Br; page 25).

The substituents chosen for the designed compounds pos­ sess different electronic, solubility and steric parameters which may affect or modify the expected biological activ­ ities.

The present work afforded the synthesis of two reported intermediates; 2-amino-6-methyl(phenyl)-4(3H)-pyrimidinones (3a,b). The work, also, yielded 23 final compounds, 15 of them are new and not reported in the literatures.

(A) The reported final compounds are:

i- 2-Alnino-5-bromo-6-phenyl-4(JH)-pyrimidinone•