Synthesis of the key intermediate, diethyl 2-acetylamino-2-(2-(4- octanoylphenyl)ethyl)propane-1,3-dioate, of the immunomodulatory agent FTY720 (fingolimod)

Norimasa Matsumoto; Ryoji Hirose; Shigeo Sasaki; Tetsuro Fujita

Journal ArticleOPEN ACCESS

Synthesis of the key intermediate, diethyl 2-acetylamino-2-(2-(4- octanoylphenyl)ethyl)propane-1,3-dioate, of the immunomodulatory agent FTY720 (fingolimod)

Chemical and Pharmaceutical Bulletin (2008) 56(4) 595-597

DOI: 10.1248/cpb.56.595

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Abstract

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). © 2008 Pharmaceutical Society of Japan.

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Matsumoto, N., Hirose, R., Sasaki, S., & Fujita, T. (2008). Synthesis of the key intermediate, diethyl 2-acetylamino-2-(2-(4- octanoylphenyl)ethyl)propane-1,3-dioate, of the immunomodulatory agent FTY720 (fingolimod). Chemical and Pharmaceutical Bulletin, 56(4), 595–597. https://doi.org/10.1248/cpb.56.595

Synthesis of the key intermediate, diethyl 2-acetylamino-2-(2-(4- octanoylphenyl)ethyl)propane-1,3-dioate, of the immunomodulatory agent FTY720 (fingolimod)

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