Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1375731 | Bioorganic & Medicinal Chemistry Letters | 2005 | 5 Pages |
Abstract
Synthetic and biological evaluation of novel diphenyloxazole derivatives containing a pyrrolidine ring, as a prostacyclin mimetic without the PG skeleton, are described. Asymmetric reduction of a ketone using a chiral Ru complex and reductive amination by NaBH4 produces four isomers of the tetrahydronaphthalene ring and the pyrrolidine ring with high stereoselectivity. FR193262 (4), (R,R)-diphenyloxazolyl pyrrolidine derivative, displays high potency and agonist efficacy at the IP receptor and has good bioavailability in rats and dogs.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Kouji Hattori, Osamu Okitsu, Seiichiro Tabuchi, Kiyoshi Taniguchi, Mie Nishio, Satoshi Koyama, Jiro Seki, Kazuo Sakane,