Application of a Sequential Multicomponent Assembly Process/Huisgen Cycloaddition Strategy to the Preparation of Libraries of 1,2,3-Triazole-Fused 1,4-Benzodiazepines

作者：Donald James R; Wood Rebekah R; Martin Stephen F^*

来源：ACS Combinatorial Science, 2012, 14(2): 135-143.

DOI：10.1021/co2002087

• triazole
• dipolar cycloaddition
• azide-alkyne
• benzodiazepine
• multicomponent reaction
• alpha-aminonitrile
• diversity oriented synthesis

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 alpha-aminonitrile chemistry.

• 出版日期2012-2