title: Design and synthesis of a selective EP4-receptor agonist. Part 4: practical synthesis and biological evaluation of a novel highly selective EP4-receptor agonist.
abstract: A practical method of synthesizing a highly selective EP4-receptor agonist 1 using Corey lactone 2 as a key intermediate was developed. Selective methanesulfonylation of the primary alcohol of the diol 8 under the newly devised conditions followed by the protection of the remaining secondary alcohol are key reactions in this new method. Further biological evaluation of 1a-b is also reported.
authors: Minase Research Institute, Ono Pharmaceutical Co., Ltd., Shimamoto, Mishima, Osaka 618-8585, Japan. to.maruyama@ono.co.jp
authors: Toru
authors: T
authors: Maruyama
authors: Shin-Itsu
authors: SI
authors: Kuwabe
authors: Yasufumi
authors: Y
authors: Kawanaka
authors: Tai
authors: T
authors: Shiraishi
authors: Yoshiyuki
authors: Y
authors: Shinagawa
authors: Kiyoto
authors: K
authors: Sakata
authors: Akiteru
authors: A
authors: Seki
authors: Yoko
authors: Y
authors: Kishida
authors: Hideyuki
authors: H
authors: Yoshida
authors: Takayuki
authors: T
authors: Maruyama
authors: Shuichi
authors: S
authors: Ohuchida
authors: Hisao
authors: H
authors: Nakai
authors: Shinsuke
authors: S
authors: Hashimoto
authors: Masanori
authors: M
authors: Kawamura
authors: Kigen
authors: K
authors: Kondo
authors: Masaaki
authors: M
authors: Toda
mesh_terms: D000818:Animals; D001773:Blood Cells / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D016753:Interleukin-10 / Q000096:biosynthesis / Q000097:blood; D008070:Lipopolysaccharides / Q000494:pharmacology; D051381:Rats; D018078:Receptors, Prostaglandin E / Q000819:agonists*; D058309:Receptors, Prostaglandin E, EP4 Subtype; D015398:Signal Transduction; D013057:Spectrum Analysis; D014409:Tumor Necrosis Factor-alpha / Q000378:metabolism
chemical_list: D008070:Lipopolysaccharides; C545650:PTGER4 protein, human; D018078:Receptors, Prostaglandin E; D058309:Receptors, Prostaglandin E, EP4 Subtype; D014409:Tumor Necrosis Factor-alpha; D016753:Interleukin-10