A convenient ‘catch and release’ synthesis of fused 2-alkylthio-pyrimidinones mediated by polymer-bound BEMP

A robust ‘catch and release’ synthesis of fused 2-alkylthio-3-substituted-pyrimidinones mediated by the polymer-bound base P-BEMP is described. This reengineered synthesis combines the efficiency of the classical synthesis (three steps, three diversity points) with the practical benefits of resin-bo...

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Bibliographic Details
Published in:Tetrahedron letters 2003-06, Vol.44 (27), p.5041-5045
Main Authors: Adams, Gregory L, Graybill, Todd L, Sanchez, Robert M, Magaard, Victoria W, Burton, George, Rivero, Ralph A
Format: Article
Language:English
Subjects:
2- tert-butylimino-2-diethylamino-1,3-dimethyl-perhydro-1,3,2-diazaphosphorine
parallel synthesis
quinazolin-4-one
quinazolinone
solid-supported reagents
thienopyrimidinone
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Summary:A robust ‘catch and release’ synthesis of fused 2-alkylthio-3-substituted-pyrimidinones mediated by the polymer-bound base P-BEMP is described. This reengineered synthesis combines the efficiency of the classical synthesis (three steps, three diversity points) with the practical benefits of resin-bound reagents. The solution-phase strategy, reagent compatibility, and the results of a representative 48-member combinatorial library are described and presented herein. Graphic
ISSN:0040-4039
1873-3581
DOI:10.1016/S0040-4039(03)01188-2