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Design and synthesis of a selective EP4-receptor agonist. Part 4: practical synthesis and biological evaluation of a novel highly selective EP4-receptor agonist |
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| Authors: | Maruyama Toru Kuwabe Shin-Itsu Kawanaka Yasufumi Shiraishi Tai Shinagawa Yoshiyuki Sakata Kiyoto Seki Akiteru Kishida Yoko Yoshida Hideyuki Maruyama Takayuki Ohuchida Shuichi Nakai Hisao Hashimoto Shinsuke Kawamura Masanori Kondo Kigen Toda Masaaki |
| Institution: | Minase Research Institute, Ono Pharmaceutical Co., Ltd., Shimamoto, Mishima, Osaka 618-8585, Japan. to.maruyama@ono.co.jp |
| 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. |
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