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Synthesis of a 2, 4, 8-trisubstituted pyrimidino[5, 4-d]pyrimidine library via sequential SNAr reactions on solid-phase
Authors:El-Araby M  Pottorf R S  Player M R
Affiliation:Drug Discovery, Johnson & Johnson Pharmaceutical Research and Develoment, L.L.C., 8 Clarke Dr., Cranbury, NJ 08512, USA. mplayer@prdus.jnj.com
Abstract:A solid-phase synthesis of 2, 4, 8-substituted pyrimidino[5, 4-d]pyrimidines involving three controlled S(N)Ar 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.
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