CRTH2 antagonist MK-7246: a synthetic evolution from discovery through development

…, ME Howard, DJ Wallace, PD O'Shea

Index: Molinaro, Carmela; Bulger, Paul G.; Lee, Ernest E.; Kosjek, Birgit; Lau, Stephen; Gauvreau, Danny; Howard, Melissa E.; Wallace, Debra J.; O'Shea, Paul D. Journal of Organic Chemistry, 2012 ,  vol. 77,  # 5  p. 2299 - 2309

Full Text: HTML

Citation Number: 24

Abstract

In this paper, we report the development of different synthetic routes to MK-7246 (1) designed by the Process Chemistry group. The syntheses were initially designed as an enabling tool for Medicinal Chemistry colleagues in order to rapidly explore structure– activity relationships (SAR) and to procure the first milligrams of diverse target molecules for in vitro evaluation. The initial aziridine opening/cyclodehydration strategy was also directly ...