Tert-Butylamine → (2S,3aS,7aS)-1-[(2S)-2-[[(1S)-1-(Ethoxycarbonyl)butyl]amino]-1-oxopropyl]octahydro-1H-indole-2-carboxylic Acid Benzyl Ester

Beteiligte Stoffe

Reaktionsschritte

EP 308 341 teaches an improved large-scale synthesis of perindopril in the form of the t-butylamine salt. (2S,3aS,7aS)-octahydroindole-2-carboxylic acid benzyl ester p-toluensulfonic salt and N-((S)-1-carbethoxybutyl)-L-alanine are reacted in the presence of triethyl amine, N,N-dicyclohexylcarbodiimide and 1-hydroxybenztriazole. After completion of the reaction, perindopril benzyl ester is obtained, which is reduced, lyophilized and then converted into a salt with t-butylamine in ethyl acetate.

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