Current Organic Chemistry - Volume 10, Issue 3, 2006

This special issue of Current Organic Chemistry is devoted to several current synthetic and biological aspects of the chemistry of diazines to illustrate the considerably increasing interest in and complexity of this research area. The wide range of the synthetic procedures and strategies recently developed and described in this issue for the syntheses of diazine derivatives may also have broader applicability in the heteroc Read More

Here we report our medicinal chemistry approach on the synthesis of the pyrazolo[4,3-e][1,2,4]triazolo[1,5- c]pyrimidines and related compounds that have permitted us to complete the SAR analyses on this class of chemical molecules. Evaluating their pharmacological profiles, we planned several structural modifications to modulate the biological activity versus the different adenosine receptor subtypes. Efforts made by ou Read More

Efficient chemical pathways leading to differently substituted 3-aminopyridazines have been reviewed with the general objective to help to design the most straightforward chemical pathways to produce libraries of compounds with largest chemical diversity. Thus 3-chloropyridazines bearing at different positions halogens may offer opportunities, when submitted two tandem of selected reactions leading to the expected compou Read More

The present review is devoted to heterocyclizations of unsaturated carbonyl compounds which result in the formation of six-membered partially hydrogenated heterocycles. Three main pathways of such reactions are discussed: syntheses of dihydropyridines by preliminary transformation of unsaturated ketone, cyclocondensations of unsaturated carbonyl compounds with nitrogen containing 1,3-binucleophiles and heterocycli Read More

A survey is provided on new synthetic pathways to pyrido[1,2-a]pyrimidinium, pyrido[1,2-a]pyrazinium, pyrido[1,2-c]pyrimidinium, and pyrido[1,2-b]pyridazinium systems and their partially saturated derivatives appeared during the recent years. Reaction mechanisms of these ring closure methodologies are also discussed. Some representative further transformations of these ring systems are also summarized. Thus, alkyla Read More

Early work on antiviral agents focused on traditional nucleoside analogues in which the base was linked to one or other of the naturally occurring sugars. Some of these were indeed shown to possess anti-metabolic properties, but it became apparent that their usefulness was severely limited by instability and poor selectivity. Since the discovery of the first successful anti-viral drug, acyclovir, in 1974 by Gertrude "Trudy" Elion, i Read More

The pyrido[4,3-b]carbazole alkaloids, ellipticine and olivacine, have been attracting considerable interest since many years due to their pronounced antitumour activity. Among the large number of structural variations of these lead compounds which have been performed in search of new agents with enhanced pharmacological profiles, a remarkable proportion of work has been devoted to the synthesis of diazine-fused carbazoles Read More

In this report, we review the C- and N-functionalization of the pyridazine nucleus via palladium-catalyzed reactions (Suzuki, Stille, Sonogashira, carbonylation, Heck, Buchwald-Hartwig) in which carbon atoms of the pyridazine nucleus are involved. The efficient use of these reactions in synthetic strategies to build up polycyclic 1,2-diazines is also included.