Process for making n-sulfonated-amino acid derivatives

C - Chemistry – Metallurgy – 07 – D

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C07D 315/00 (2006.01)

Patent

CA 2566191

This invention relates to a process for preparing optically active .alpha. - amino acid substrates which are used to make potent lethal factor (LF) inhibitors for the treatment of anthrax. This invention further relates to a process for synthesis of potent LF-inhibitors for the treatment of anthrax. Specifically, the invention concerns a novel, high-yielding and highly enantioselective asymmetric hydrogenation reaction of a tetrasubstituted ene- sulfonamide acid or ester.

La présente invention concerne un procédé d'élaboration de substrats optiquement actifs d'acide A-aminé utilisé pour la fabrication de puissants inhibiteurs de facteur létal (LF) destinés au traitement de la maladie du charbon. L'invention concerne également un procédé de synthèse de puissants inhibiteurs de facteur létal pour le traitement de la maladie du charbon. L'invention concerne plus particulièrement une nouvelle réaction à haut rendement et hautement énantiosélective d'hydrogénation asymétrique d'acide ou d'ester d'ène-sulfonamide tétra-substitué.

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