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Combinatorial Chemistry & High Throughput Screening


ISSN (Print): 1386-2073
ISSN (Online): 1875-5402

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

Author(s): M. El-Araby, R. S. Pottorf and M. R. Player

Volume 7 , Issue 5 , 2004

Page: [413 - 421] Pages: 9

DOI: 10.2174/1386207043328571

Price: $65


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.

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

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