Issue 3, 2015

Expanding the scope of fused pyrimidines as kinase inhibitor scaffolds: synthesis and modification of pyrido[3,4-d]pyrimidines

Abstract

Fused pyrimidine cores are privileged kinase scaffolds, yet few examples of the 2-amino-pyrido[3,4-d]pyrimidine chemotype have been disclosed in the context of kinase inhibitor programs. Furthermore, no general synthetic route has been reported to access 2-amino-pyrido[3,4-d]pyrimidine derivatives. Here we report a versatile and efficient chemical approach to this class of molecules. Our strategy involves the concise preparation of 8-chloro-2-(methylthio)pyrido[3,4-d]pyrimidine intermediates and their efficient derivatisation to give novel compounds with potential as kinase inhibitors.

Graphical abstract: Expanding the scope of fused pyrimidines as kinase inhibitor scaffolds: synthesis and modification of pyrido[3,4-d]pyrimidines

Supplementary files

Article information

Article type
Paper
Submitted
21 Oct 2014
Accepted
06 Nov 2014
First published
19 Nov 2014

Org. Biomol. Chem., 2015,13, 893-904

Author version available

Expanding the scope of fused pyrimidines as kinase inhibitor scaffolds: synthesis and modification of pyrido[3,4-d]pyrimidines

P. Innocenti, H. Woodward, L. O'Fee and S. Hoelder, Org. Biomol. Chem., 2015, 13, 893 DOI: 10.1039/C4OB02238F

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