A versatile PIFA-mediated approach to structurally diverse pyrrolo(benzo)diazepines from linear alkynylamides |
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Authors: | Leticia M. Pardo,Esther Domí nguez |
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Affiliation: | Departamento de Química Orgánica II, Facultad de Ciencia y Tecnología (ZTF/FCT), Universidad del País Vasco/Euskal Herriko Unibertsitatea (UPV/EHU), PO Box 644, 48080 Bilbao, Spain |
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Abstract: | The addition of the hypervalent iodine reagent PIFA [phenyliodine(III) bis(trifluoroacetate)] to a series of properly substituted N-(3-aminopropyl)alkynylamides results in the efficient formation of a functionalized 5-aroyl-2-pyrrolidinone skeleton. By proper manipulations of the N(1)-substituents, through consecutive deprotection and/or reductive amination steps, a second cyclization process occurs yielding the target heterocycles. As it will be disclosed, the overall process is open to structural modifications that gives rise to a series of pyrrolo(benzo)diazepine derivatives. |
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Keywords: | Hypervalent iodine Alkynylamides PIFA Reductive amination Diazepines |
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