An intramolecular inverse electron demand Diels-Alder approach to annulated α-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 α-carbolines. Beginning with various isatins and alkynyl dienophiles, a pilot-scale library of eighty-eight α-carbolines was prepared by using this robust methodology for biological evaluation.

SUBMITTER: Ma Z 

PROVIDER: S-EPMC3388871 | biostudies-literature | 2012

REPOSITORIES: biostudies-literature