An efficient total synthesis of a sphingosine-1-phosphate receptor agonist KRP-203 |
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| Authors: | Masao Chino Masatoshi Kiuchi Kunitomo Adachi |
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| Institution: | Chemistry Laboratory, Pharmaceuticals Research Division, Mitsubishi Tanabe Pharma Corporation, 1000, Kamoshida, Aoba-ku, Yokohama 227-0033, Japan |
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| Abstract: | An efficient total synthesis of the S1P1 agonist, KRP-203, is described. The key step involves the conjugate addition of diethyl acetamidomalonate to a styrene compound to give the core structure of KRP-203. Multigram quantities of the targeted KRP-203, sufficient for several biological studies, were obtained in six steps with an overall yield of 58%. |
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