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Application of a sequential multicomponent assembly process/huisgen cycloaddition strategy to the preparation of libraries of 1,2,3-triazole-fused 1,4-benzodiazepines.


ABSTRACT: A strategy featuring a multicomponent assembly process followed by an intramolecular azide-alkyne dipolar (Huisgen) cycloaddition was implemented for the facile synthesis of three different 1,2,3-triazolo-1,4-benzodiazepine scaffolds. A diverse library of 170 compounds derived from these scaffolds was then created through N-functionalizations, palladium-catalyzed cross-coupling reactions, and several applications of ?-aminonitrile chemistry.

SUBMITTER: Donald JR 

PROVIDER: S-EPMC3278535 | biostudies-other | 2012 Feb

REPOSITORIES: biostudies-other

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Application of a sequential multicomponent assembly process/huisgen cycloaddition strategy to the preparation of libraries of 1,2,3-triazole-fused 1,4-benzodiazepines.

Donald James R JR   Wood Rebekah R RR   Martin Stephen F SF  

ACS combinatorial science 20120201 2


A strategy featuring a multicomponent assembly process followed by an intramolecular azide-alkyne dipolar (Huisgen) cycloaddition was implemented for the facile synthesis of three different 1,2,3-triazolo-1,4-benzodiazepine scaffolds. A diverse library of 170 compounds derived from these scaffolds was then created through N-functionalizations, palladium-catalyzed cross-coupling reactions, and several applications of α-aminonitrile chemistry. ...[more]

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