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Synfacts 2010(2): 0140-0140
DOI: 10.1055/s-0029-1219027
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
C. Molinaro*, G. Hughes et al. *
Merck Frosst Center for Therapeutic Research, Kirkland, Canada and , Merck Research Laboratories, Rahway, USA
Weitere Informationen
Publikationsverlauf
Publikationsdatum:
21. Januar 2010 (online)
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).