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.