A simple stereoselective synthesis and biological evaluation of FR181157: orally active prostacyclin mimetic

  • Bioorg Med Chem Lett. 2003 Dec 15;13(24):4277-9. doi: 10.1016/j.bmcl.2003.09.054.
Kouji Hattori  1 ,  Seiichiro Tabuchi ,  Osamu Okitsu ,  Kiyoshi Taniguchi
Affiliations
  • 1. Medicinal Chemistry Research Laboratories, Fujisawa Pharmaceutical Co. Ltd, 1-6, Kashima 2-Chome, Yodogawa-Ku, Osaka, Japan. [email protected]
PMID: 14643308 DOI: 10.1016/j.bmcl.2003.09.054
Abstract

Synthetic method of a novel prostaglandin (PG) mimetic: FR181175 without PG skeleton are described. The key to success is creation of a chiral epoxide using Sharpless AD reaction with high ee yield. FR181157 shows high potency and agonist efficacy at the IP receptor and has good bioavailability.

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