American Chemical Society
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A Practical Synthesis of m-Prostaglandin E Synthase-1 Inhibitor MK-7285

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journal contribution
posted on 2009-10-16, 00:00 authored by Francis Gosselin, Stephen Lau, Christian Nadeau, Thao Trinh, Paul D. O’Shea, Ian W. Davies
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.