Facile access to a heterocyclic, sp(3)-rich chemical scaffold via a tandem condensation/intramolecular nitrone-alkene [3+2] cycloaddition strategy

Facile access to a heterocyclic, sp(3)-rich chemical scaffold via a tandem condensation/intramolecular nitrone-alkene [3+2] cycloaddition strategy

A heterocyclic, sp(3)-rich chemical scaffold was synthesised in just 6 steps via a highly regio- and diastereo-selective tandem nitrone formation/intramolecular nitrone-alkene [3+2] cycloaddition reaction. A library of 543 lead-like compounds based on the scaffold core has been produced.

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Bibliographische Detailangaben
Veröffentlicht in:Chemical communications (Cambridge, England) England), 2015-08, Vol.51 (64), p.12867-12870
Hauptverfasser: Rawling, M J, Storr, T E, Bawazir, W A, Cully, S J, Lewis, W, Makki, M S I T, Strutt, I R, Jones, G, Hamza, D, Stockman, R A
Format: Artikel
Sprache:eng
Schlagworte:
Alkenes - chemistry
Cycloaddition Reaction
Heterocyclic Compounds - chemistry
Nitrogen Oxides - chemistry
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Beschreibung
Zusammenfassung:A heterocyclic, sp(3)-rich chemical scaffold was synthesised in just 6 steps via a highly regio- and diastereo-selective tandem nitrone formation/intramolecular nitrone-alkene [3+2] cycloaddition reaction. A library of 543 lead-like compounds based on the scaffold core has been produced.
ISSN:1364-548X
DOI:10.1039/c5cc05070g