Regioselective cross-coupling reactions and nucleophilic aromatic substitutions on a 5,7-dichloropyrido[4,3-d]pyrimidine scaffold |
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Authors: | Mi-Yeon Jang Ling-Jie Gao |
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Institution: | a REGA Institute, Laboratory of Medicinal Chemistry, Minderbroedersstraat 10, 3000 Leuven, Belgium b 4AZA Bioscience, Department of Medicinal Chemistry, Kapucijnenvoer 33, 3000 Leuven, Belgium |
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Abstract: | The synthesis of a 5,7-dichloropyrido4,3-d]pyrimidine scaffold is described. The chlorine at position 5 can selectively be displaced by different palladium-catalyzed cross-coupling reactions and nucleophilic aromatic substitutions. In the subsequent step, the chlorine at position 7 can be further derivatized. The described synthetic sequence allows for the construction of a diverse pyrido4,3-d]pyrimidine library with structural variations at positions 5 and 7. |
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Keywords: | Pyrido[4 3-d]pyrimidines Heterocycles Combinatorial chemistry Library |
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