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

…, ME Howard, DJ Wallace, PD O'Shea

文献索引：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

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被引用次数: 24

摘要

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 ...