title: 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.
authors.affiliation: Department of Chemistry and the Center for Chemical Methodology and Library Development (CMLD-BU), Boston University, 590 Commonwealth Avenue, Boston, Massachusetts 02215.
authors.forename: Zhiyuan
authors.initials: Z
authors.lastname: Ma
authors.forename: Feng
authors.initials: F
authors.lastname: Ni
authors.forename: Grace H C
authors.initials: GH
authors.lastname: Woo
authors.forename: Sie-Mun
authors.initials: SM
authors.lastname: Lo
authors.forename: Philip M
authors.initials: PM
authors.lastname: Roveto
authors.forename: Scott E
authors.initials: SE
authors.lastname: Schaus
authors.forename: John K
authors.initials: JK
authors.lastname: Snyder