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Synthesis of a 2, 4, 8-Trisubstituted Pyrimidino[5, 4-d]Pyrimidine Library via Sequential SNAr Reactions on Solid-Phase

[ Vol. 7 , Issue. 5 ]


M. El-Araby, R. S. Pottorf and M. R. Player   Pages 413 - 421 ( 9 )


A solid-phase synthesis of 2, 4, 8-substituted pyrimidino[5, 4-d]pyrimidines involving three controlled SNAr reactions has been developed. Exploration of different heterocyclic starting materials and resin-bound intermediates is highlighted. The preferred method starts with the treatment of resin-bound anilines with 2, 4, 8-trichloropyrimidino[5, 4-d]pyrimidine. This intermediate is subsequently treated with various amines in two steps to yield the final products. The scope of each diversity step was determined and a library of 16, 000 compounds was synthesized.


pyrimidinopyrimidine, kinase inhibitor, atp analogue, combinatorial, parallel synthesis, snar


Drug Discovery, Johnson&Johnson Pharmaceutical Research and Develoment, L.L.C., 8 Clarke Dr.,Cranbury, NJ 08512, USA.

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