Litcius/Paper detail

Bisketene Equivalents as Diels–Alder Dienes

Isuru Dissanayake, Jacob D. Hart, Emma C. Becroft, Christopher J. Sumby, Christopher G. Newton

2020Journal of the American Chemical Society30 citationsDOIOpen Access PDF

Abstract

2,5-Bis(tert-butyldimethylsilyloxy)furans are established as vicinal bisketene equivalents for application as dienes in the Diels–Alder reaction. Cycloaddition with olefinic dienophiles, under exceptionally mild conditions, enables convergent access to highly substituted para-hydroquinones in unprotected form via a one-pot Diels–Alder/ring-opening/tautomerization sequence. The synthesis of para-benzoquinones from acetylenic dienophiles, including benzynes, is also demonstrated, and 2,5-bis(tert-butyldimethylsilyloxy)pyrroles are established as competent dienes for the synthesis of para-iminoquinones. Application in natural product synthesis enables gram-scale access to the neuroprotective agent (±)-indanostatin.

Topics & Concepts

ChemistryEquivalentDiels–Alder reactionOrganic chemistryCatalysisBiochemistryCancer Treatment and PharmacologyCyclization and Aryne ChemistryAsymmetric Synthesis and Catalysis