| Reference | [1]. Crestey, François & Hooyberghs, Geert & Kristensen, Jesper. (2012).<br />
Concise synthesis of new bridged-nicotine analogues.<br />
Tetrahedron. 68. 1417-1421. 10.1016/j.tet.2011.12.029.<br />
This study describes a very efficient strategy for the synthesis of two new bridged-nicotine analogues. Starting from either 4- or 3-chloropyridine the desired tricyclic ring systems are accessed in just three steps in 23% and 40% overall yield, respectively.<br />
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[2]. Expanding the scope of fused pyrimidines as kinase inhibitor scaffolds: synthesis and modification of pyrido[3,4-d]pyrimidines<br />
Organic & Biomolecular Chemistry; OB-ART-10-2014-002238; 21-Oct-2014<br />
Innocenti, Paolo; Institute of Cancer Research, Medicinal Chemistry Woodward, Hannah; Institute of Cancer Research, Medicinal Chemistry O Fee, Lisa; Institute of Cancer Research, Cancer Therapeutics Hoelder, Swen; Institute of Cancer Research, Medicinal Chemistry<br />
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.
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