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

Gosselin, Francis; Lau, Stephen; Nadeau, Christian; Trinh, Thao; O’Shea, Paul D.; Davies, Ian W.

doi:10.1021/jo901798d.s001

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

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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.

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Practical Synthesis convergent assembly mPGE synthase cyclization cyanation imidazole synthesis Synthase Inhibitor route features MK core phenanthrene unit inhibitor

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CC BY-NC 4.0

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

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