Selective C-acylation of 2-aminoimidazo[1,2-a]pyridine: application to the synthesis of imidazopyridine-fused [1,3]diazepinones |
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| Authors: | Masurier Nicolas Aruta Roberta Gaumet Vincent Denoyelle Séverine Moreau Emmanuel Lisowski Vincent Martinez Jean Maillard Ludovic T |
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| Institution: | Institut des Biomolécules Max Mousseron, UMR 5247, CNRS, Universités Montpellier I et II, UFR des Sciences Pharmaceutiques et Biologiques, 15 Avenue Charles Flahault, 34093 Montpellier Cedex 5, France. nicolas.masurier@univ-montp1.fr |
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| Abstract: | A series of 20 optically pure 3,4-dihydro-5H-pyrido1',2':1,2]imidazo4,5-d]1,3]diazepin-5-ones which form a new family of azaheterocycle-fused 1,3]diazepines were synthesized in four steps with 17-66% overall yields. The key step consists of a selective C-acylation reaction of easily accessible 2-aminoimidazo1,2-a]pyridine at C-3. |
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