Abstract: A method for preparing 1,2-dihydroquinolines that is more flexible than the Skraup reaction is provided. The method comprises treating an ortho-alkenyl aniline with a ketone in the presence of a Lewis acid. Novel intermediates and products of this method useful as steroid receptor modulators, as well as pharmaceutical compositions and methods of use thereof are also claimed.
Type:
Grant
Filed:
October 15, 1999
Date of Patent:
January 30, 2001
Assignee:
Ligand Pharmacueticals Incorparated
Inventors:
James P. Edwards, Todd K. Jones, Josef D. Riggenberg, Erick M. Carreira