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16.22.4.1.1.1.2.2 Variation 2: From 2,6-Disubstituted 4-Aminopyrimidine-5-carboxamides

DOI: 10.1055/sos-SD-016-01695

Ishikawa, T.Science of Synthesis, (2004161371.

4-Aminopyrimidine-5-carboxamides 108, obtained by hydrolysis of the corresponding carbonitriles,[‌104‌] are key structures in the synthesis of pyrimidopyrimidines. Heating them with triethyl orthoformate in the presence of an acid anhydride affords pyrimido[4,5-d]pyrimidin-4-ol systems 109, in which the acid anhydride is used to remove the ethanol formed during the reaction (Scheme 76).[‌102‌,‌104‌,‌105‌,‌107‌,‌130‌‌132‌]

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