Abstract
Electron‐deficient propargylic alcohols (EWG = CN, C(O)Ph, CO2Me, C(O)NH2) under catalyst‐free mild conditions are annulated with Δ1‐pyrrolines to afford functionalized hexahydropyrrolo[2,1‐b]oxazoles, mostly in 19–93 % yield. The synthesis is stereoselective with respect to disposition of functionalized ethenyl group relative to the condensed heterocyclic system thus formed in most cases. This methodology provides a simple one‐pot access to a novel family of synthetically and pharmaceutically prospective.
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