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Solid-Phase Synthesis of Quinazoline-2,4-Diones and Their Analogues from Resin-Bound Compounds with Primary Amines

[ Vol. 6 , Issue. 6 ]


Shingo Makino   Pages 625 - 632 ( 8 )


Solid-phase organic synthesis of heterocyclic compounds on solid-support has been a focus of recent investigations because of the potential applicability of these compounds toward a variety of drug targets. Among the various heterocycles, we have been especially interested in quinazoline-2,4-diones because of the wide range of their bioactivities. Therefore, in this article we review methods for the solid-phase synthesis of quinazoline-2,4-diones and their analogues. Since all of these heterocycles can be speedily derivatized from resin-bound primary amines, incorporating the amines at the 3N-position of quinazoline-2,4-diones or corresponding positions of its analogues, it becomes possible to efficiently compare the bioactivities of these quinazoline-2,4-diones and their analogues. Various methods of solid-phase synthesis described herein should be practical and useful tools for the medicinal chemist in supporting drug discovery initiatives.


Solid-phase synthesis, resin-bound, heterocycle, quinazoline, quinazoline-2, 4-dione


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