- PROCESS FOR PREPARATION OF FINGOLIMOD
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The present invention provides a process for preparation of fingolimod, a compound of Formula I or a pharmaceutically acceptable salt thereof, free of regioisomeric impurity compound of Formula IA
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- 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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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).
- Matsumoto, Norimasa,Hirose, Ryoji,Sasaki, Shigeo,Fujita, Tetsuro
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experimental part
p. 595 - 597
(2009/04/11)
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- PROCESS FOR PREPARING 2-AMINO MALONIC ACID DERIVATIVES AND 2-AMINO-1,3 - PROPANEDIOL DERIVATIVES, AND INTERMEDIATES FOR PREPARING THE SAME
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A process for preparing 2-amino malonic acid derivatives of formula (1): wherein A is linear or branched chain alkylene having from 1 to 10 carbon atoms, R1 is linear or branched chain alkyl having from 2 to 20 carbon atoms, R2 and R3 are the same or different, and are lower alkyl or aralkyl, and R4 is a protecting group, which process comprises the steps of reducing a compound of formula (6): wherein A is linear or branched chain alkylene having from 1 to 10 carbon atoms, R1 is linear or branched chain alkyl having from 2 to 20 carbon atoms, R2 and R3 are the same or different, and are lower alkyl or aralkyl, and R4 is a protecting group.
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