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A Synthesis of Alstonlarsine A via Alstolucines B and F Demonstrates the Chemical Feasibility of a Proposed Biogenesis

Griffin L. Barnes, Allen Y. Hong, Christopher D. Vanderwal

2022Angewandte Chemie International Edition10 citationsDOIOpen Access PDF

Abstract

We offer a new biogenetic proposal for the origin of the complex alkaloid alstonlarsine A, through rearrangement of the Strychnos alkaloids alstolucines B and F. Further, we provide evidence of the chemical feasibility of this proposal in the facile conversion of synthetic alstolucines into alstonlarsine A through a short, efficient sequence of N-methylation, β-elimination, and a cascade 1,7-hydride shift/Mannich cyclization. We believe that this is the first biogenetic proposal involving the "tert-amino effect", a hydride-shift-based internal redox trigger of a Mannich cyclization. A further interesting feature of the cascade is that its stereochemical outcome most likely originates in conformational preferences during the hydride shift.

Topics & Concepts

HydrideBiogenesisChemistryCascadeCombinatorial chemistryStereochemistrySequence (biology)StrychnosAlkaloidOrganic chemistryBiochemistryGeneHydrogenChromatographyAlkaloids: synthesis and pharmacologyTraditional and Medicinal Uses of AnnonaceaeChemical synthesis and alkaloids
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