Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
Notes
Synthesis of the Key Intermediate, Diethyl 2-Acetylamino-2-(2-(4-octanoylphenyl)ethyl)propane-1,3-dioate, of the Immunomodulatory Agent FTY720 (Fingolimod)
Norimasa MatsumotoRyoji HiroseShigeo SasakiTetsuro Fujita
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2008 年 56 巻 4 号 p. 595-597

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The key intermediate, diethyl 2-acetylamino-2-(2-(4-octanoylphenyl)ethyl)propane-1,3-dioate (13), for the immunomodulatory agent FTY720 (2: fingolimod) was synthesized via Michael addition of diethyl(acetylamino)malonate (6) to 4-octanoylstyrene (12).

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© 2008 The Pharmaceutical Society of Japan
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