Development of Scalable Conditions for the Ugi Reaction-Application to the Synthesis of (R)-Lacosamide
The Ugi reaction is applied for the preparation of (R)-lacosamide, an important drug for the treatment of epilepsy. To this end, key issues associated with the Ugi reaction, such as a practical preparation of the foul-smelling isocyanide as well as the efficient introduction of chirality via a cheap and easily removable chiral directing group, were solved. Enantiomerically pure (>99.9% ee) drug substance meeting all required purity specifications is prepared in operationally simple four steps in 40% overall yield from the commodity chemical benzylamine.
Wehlan, Hermut,Oehme, Jan,Sch?fer, Alexander,Rossen, Kai
p. 1980 - 1986
(2016/01/09)
PROCESS FOR THE PRODUCTION OF N-SUBSTITUTED 2-(ACETYLAMINO)-N'-BENZYL-3-METHOXYPROPANAMIDES
A process for the production of N-substituted 2-(acetylamino)-N'-benzyl-3-methoxypropanamides and subsequent treatment with acids is described. This process can be used for the production of (R)-Lacosamide.
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Page/Page column 26; 27
(2013/06/05)
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