Document Detail


A practical synthesis of m-prostaglandin E synthase-1 inhibitor MK-7285.
MedLine Citation:
PMID:  19777997     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
Francis Gosselin; Stephen Lau; Christian Nadeau; Thao Trinh; Paul D O'Shea; Ian W Davies
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  The Journal of organic chemistry     Volume:  74     ISSN:  1520-6904     ISO Abbreviation:  J. Org. Chem.     Publication Date:  2009 Oct 
Date Detail:
Created Date:  2009-10-09     Completed Date:  2009-12-29     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  2985193R     Medline TA:  J Org Chem     Country:  United States    
Other Details:
Languages:  eng     Pagination:  7790-7     Citation Subset:  IM    
Affiliation:
Department of Process Research, Merck Frosst Centre for Therapeutic Research, 16711 Route Transcanadienne, Kirkland, Qu??bec, Canada H9H 3L1. francis_gosselin@merck.com
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MeSH Terms
Descriptor/Qualifier:
Cyclization
Enzyme Inhibitors / chemical synthesis*,  chemistry*
Heterocyclic Compounds with 4 or More Rings / chemical synthesis*,  chemistry*
Intramolecular Oxidoreductases / chemistry*
Molecular Structure
Chemical
Reg. No./Substance:
0/Enzyme Inhibitors; 0/Heterocyclic Compounds with 4 or More Rings; 0/MK-7285; EC 5.3.-/Intramolecular Oxidoreductases; EC 5.3.99.3/prostaglandin-E synthase

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