Organic Letters · 2018 · 18 citations · 56 references
PharmacyChemistryMedicinal ChemistryDrug DiscoveryOrganic ChemistrySynthetic Medicinal ChemistryDiversity-oriented SynthesisHeterocycle SynthesisHeterocyclic ChemistryMacrocycle SynthesisOrganic SynthesisRetrosynthetic AnalysisAsymmetric Heterocycle SynthesisAza-diels-alder ReactionAzetidine ChemistrySpiroheterocycle SynthesisStereoselectivityStereoselectivity ControlStereoselectivity OptimizationTethered Analogues
A range of novel (poly)cyclic alkaloids incorporating an unprecedented 1,5-diazaspiro[2.4]heptane core that carry a spiro NH aziridine moiety and a 7-vinyl group are constructed from the thermal reaction of vinyl azides with tethered alkenes. Vinyl azides are converted to 2H-azirines in situ, which serve as enophiles for intramolecular imino-ene reactions with suitable alkenes. High stereoselectivity and specificity have been achieved for this novel intramolecular imino-ene reaction of azirines.
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