Petasis three-component reactions for the synthesis of diverse heterocyclic scaffolds

Peng Wu*, Thomas E. Nielsen

*Corresponding author for this work

Research output: Contribution to journalJournal articleResearchpeer-review


The Petasis three-component reaction (PR) of hydroxy aldehydes, amines and boronic acids is an important multi-component reaction for the synthesis of structurally diverse scaffolds and biologically interesting small molecules. The reaction has been significantly explored in the past decade, and many new variants have emerged, such as asymmetric, traceless and four-component approaches. The excellent stereoselectivity, high yield and broad functional group tolerance altogether make this reaction ideal for fragment and compound collection synthesis, since orthogonal chemical handles can be incorporated for subsequent scaffold formation and appendage modification. Herein we present a selection of recent variations on the PR theme for the synthesis of scaffolds of relevance to medicinal chemistry.
Original languageEnglish
JournalDrug Discovery Today: Technologies
Pages (from-to)27-33
Number of pages7
Publication statusPublished - 2018

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