Pyrido[2,3-d]pyrimidines represent a broad class of annelated uracils of natural occurrence, which has received considerable attention over the past years due to its wide range of biological activities. Compounds with this ring system have diverse pharmacological activity such as antibacterial, antitumour, cardiotonic, hepatoprotective, antihypertensive and antibronchitics.Some of them exhibit antiallergic, antimalarial and analgesicproperties, and also act as inhibitors of adenosine kinase.
In this thesis, in order todevelop efficient and simple methods for preparation of potentially biologically important heterocyclic derivatives, we designed convenient method for synthesizing new pyrido[2,3-d]pyrimidinone derivatives.
Atfirst, new derivatives of 6-(Inden-2-yl)-pyrido[2,3-d]pyrimidinones 2-1(a-e) were synthesized via Michael addition followed by cyclization reaction of ethyl2-(2-hydroxy-1,3-dioxo-2,3-dihydro-1H-inden-2-yl)acrylate 3-1and aminouracils3-2(a-e)in DMF at 100 oC. (Scheme 1)