Process for industrial synthesis of perindopril and its...

C - Chemistry – Metallurgy – 07 – K

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530/1.02, 530/5.

C07K 5/06 (2006.01) C07K 1/02 (2006.01) C07K 5/02 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1336348

Procédé de synthèse industrielle du perindopril caractérisé en ce que l'on condense l'acide perhydroindole carboxylique - 2 (2S, 3aS, 7aS), après protection du groupement carboxyle avec la N - [(S) carbéthoxy - 1 butyl] - (S) alanine, le produit résultant de la condensation étant ensuite soumis à déprotection du carboxyle porté par l'hétérocycle. L'acide perhydroindole carboxylique - 2 (2S, 3aS, 7aS), et la N - [(S) carbéthoxy - 1 butyl] - (S) alanine, sont eux-mêmes obtenus dans d'excellentes conditions respectivement à partir de l'acide indole carboxylique - 2, et de la L - alanine, tous deux industriellement disponibles.

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