Combining the petasis 3-component reaction with multiple modes of cyclization: A build/couple/pair strategy for the synthesis of densely functionalized small molecules
Reference: ACS Combinatorial Science (2015) 17: 19-23.

A build/couple/pair strategy for the synthesis of complex and densely functionalized small molecules is presented. The strategy relies on synthetically tractable building blocks (build), that is, diversely substituted hydrazides, a-hydroxy aldehydes, and boronic acids, which undergo Petasis 3-component reactions (couple) to afford densely functionalised anti-hydrazido alcohols. The resulting scaffolds can subsequently be converted via chemoselective cyclization reactions (pair), including intramolecular Diels-Alder or Ru-alkylidene catalysed ring-closing metathesis, into sets of structurally diverse heterocycles in good yields in only 3-4 steps.

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Flagstad T., Hansen M. R., Le Quementt S. T., Givskov M., Nielsen T.E.