Synthesis and biological evaluation of optically active Ki16425

T Sato, K Sugimoto, A Inoue, S Okudaira, J Aoki…

文献索引：Sato, Takanao; Sugimoto, Kenji; Inoue, Asuka; Okudaira, Shinichi; Aoki, Junken; Tokuyama, Hidetoshi Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 13 p. 4323 - 4326

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被引用次数: 7

摘要

An enantionselective synthesis of both enantiomers of Ki16425, which possesses selective LPA antagonistic activity, was achieved. The isoxazole core was constructed by a 1, 3- dipolar cycloaddition of nitrile oxide with alkyne and condensation with the optically active α- phenethyl alcohol segment, which was prepared by an enantioselective reduction of arylmethylketone. Biological evaluation of both enantiomers of Ki16425 revealed that the ( ...