Synthetic Small Molecule GLP-1 Secretagogues Prepared by Means of a Three-Component Indole Annulation Strategy

Oleg G. Chepurny
Colin A. Leech
Martin Tomanik
Maria C. DiPoto

Oleg Chepurny;Colin Leech;Martin Tomanik;Maria DiPoto;Hui Li;Xinping Han;Qinghe Meng;Robert Cooney;Jimmy Wu;George Holz


Rational assembly of small molecule libraries for purposes of drug discovery requires an efficient approach in which the synthesis of bioactive compounds is enabled so that numerous structurally related compounds of a similar basic formulation can be derived. Here, we describe (4 + 3) and (3 + 2) indole annulation strategies that quickly generate complex indole heterocycle libraries that contain novel cyclohepta- and cyclopenta[b]indoles, respectively. Screening of one such library comprised of