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An intramolecular inverse electron demand Diels-Alder approach to annulated ?-carbolines.


ABSTRACT: Intramolecular inverse electron demand cycloadditions of isatin-derived 1,2,4-triazines with acetylenic dienophiles tethered by amidations or transesterifications proceed in excellent yields to produce lactam- or lactone-fused ?-carbolines. Beginning with various isatins and alkynyl dienophiles, a pilot-scale library of eighty-eight ?-carbolines was prepared by using this robust methodology for biological evaluation.

PROVIDER: S-EPMC3388871 | BioStudies | 2012-01-01T00:00:00Z

REPOSITORIES: biostudies

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