Synthesis of the Key Intermediate, Diethyl 2-Acetylamino-2-(2-(4-octanoylphenyl) ethyl) propane-1, 3-dioate, of the Immunomodulatory Agent FTY720 (Fingolimod)

N Matsumoto, R Hirose, S Sasaki, T Fujita

Index: Matsumoto, Norimasa; Hirose, Ryoji; Sasaki, Shigeo; Fujita, Tetsuro Chemical and Pharmaceutical Bulletin, 2008 , vol. 56, # 4 p. 595 - 597

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Citation Number: 11

Abstract

Members of our group previously isolated a potent im- munosuppressant, ISP-I (1) (Chart 1), from the culture broth of Isaria sinclairii (ATCC24400), and showed that it could suppress both lymphocyte proliferation in the mouse allo- geneic mixed lymphocyte reaction (MLR) system in vitro and generation of allo-reactive cytotoxic T lymphocytes in mice in vivo.5) Compound 1 is identical with the antifungal antibiotics myriocin6,7) and thermozymocidin,8,9) which ...