A Practical Synthesis of m-Prostaglandin E Synthase-1 Inhibitor MK-7285
A Practical Synthesis of m-Prostaglandin E Synthase-1 Inhibitor MK-7285
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DOI：
10.1021/jo901798d
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发表时间：
2009-10-16
影响因子：
3.6
通讯作者：
Davies, Ian W.
中科院分区：
文献类型：
--
作者：
Gosselin, Francis;Lau, Stephen;Davies, Ian W.
介绍了一种实用的、无层析的MPGe合成酶I抑制剂MK-7285的合成方法。该路线的特点是，通过酰胺导向的邻位金属化和邻近诱导的阴离子环化，核心菲单元聚合组装，然后是咪唑合成和后期氰化。
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.