A practical synthesis of m-prostaglandin E synthase-1 inhibitor MK-7285

…, S Lau, C Nadeau, T Trinh, PD O'Shea…

Index: Gosselin, Francis; Lau, Stephen; Nadeau, Christian; Trinh, Thao; O'Shea, Paul D.; Davies, Ian W. Journal of Organic Chemistry, 2009 , vol. 74, # 20 p. 7790 - 7797

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Citation Number: 22

Abstract

A practical, kilogram-scale chromatography-free synthesis of mPGE synthase I inhibitor MK- 7285 is described. The route features a convergent assembly of the core phenanthrene unit via amide-directed ortho-metalation and proximity-induced anionic cyclization, followed by imidazole synthesis and late-stage cyanation.