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, M. R. Player

Journal Name: Combinatorial Chemistry & High Throughput Screening
Accelerated Technologies for Biotechnology, Bioassays, Medicinal Chemistry and Natural Products Research

Volume 7 , Issue 5 , 2004

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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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Article Details

Year: 2004
Page: [413 - 421]
Pages: 9
DOI: 10.2174/1386207043328571
Price: $65

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