In a series of recent reports, we have described the biological activities and the syntheses of a variety of potent GnRH antagonists of the 2-arylindole class. 1., , , , , and Initially, these structures were prepared via the Fisher indole method, 1., , , , , , and 2. but then, ultimately, we were drawn to the elegant approach of Larock. 3. and 4. During the evolution of this medicinal chemistry effort, we became intrigued at the biological implication of replacing the indole core in ...
