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A high-yielding, stereoselective and extraordinarily complexity-generating Petasis 3-component/intramolecular Diels-Alder reaction has been developed. In combination with ROM-RCM, rapid access to complex sp 3 -rich heterocyclic scaffolds amenable to subsequent functionalization and library synthesis is provided.

Diastereoselective synthesis of novel heterocyclic scaffolds through tandem Petasis 3-component/intramolecular Diels–Alder and ROM–RCM reactions