A general approach toward the synthesis of 8-acylamidopyrazolo[1,5-a]-1,3,5-triazines |
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| Authors: | Pierre Raboisson Dominique SchultzClaire Lugnier Romain MathieuJean-Jacques Bourguignon |
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| Affiliation: | a Laboratoire de Pharmacochimie de la Communication Cellulaire (CNRS, UMR 7081), Faculté de Pharmacie, 74 route du Rhin, BP24, 67401 Illkirch Cedex, France
b Laboratoire de Pharmacologie et de Physico-Chimie des Interactions Cellulaires et Moléculaires (CNRS, UMR 7034), Faculté de Pharmacie, 74 route du Rhin, BP24, 67401 Illkirch Cedex, France |
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| Abstract: | An expedient synthesis of 8-acylamidopyrazolo[1,5-a]-1,3,5-triazines was developed by treating 8-amino-4-[N-(4-aminophenyl)-N-(methyl)amino]pyrazolo[1,5-a]-1,3,5-triazine with various acyl chlorides following by the displacement of the so-formed N-(methyl)-N-[4-(acylamido)phenyl]amino leaving group with various amines. Applications to high-throughput synthesis are suggested. |
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| Keywords: | pyrazolo[1,5-a]-1,3,5-triazine adenine bioisoster activating group |
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