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Synfacts 2010(2): 0140-0140  
DOI: 10.1055/s-0029-1219027
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of EP4 Antagonist MF-310

Contributor(s): Philip Kocienski
C. Molinaro*, G. Hughes et al. *
Merck Frosst Center for Therapeutic Research, Kirkland, Canada and , Merck Research Laboratories, Rahway, USA
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Publication History

Publication Date:
21 January 2010 (online)

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Significance

The binding of prostaglandin E4 to its receptor EP4 is a key event in neuronal function, female reproduction, vascular hypertension, tumorigenesis, kidney function and inflammation. MF-310 is a potent and selective inhibitor of the EP4 receptor under development for the treatment of chronic inflammation. The chromtography-free, multikilogram-scale synthesis depicted features an electronically controlled regioselective succinimide reduction (E → F).