Process for preparing pharmacologically acceptable salts of...

Details Process for preparing pharmacologically acceptable salts of... Process for preparing pharmacologically acceptable salts of...

C - Chemistry, Metallurgy

07

K

C07K 5/062 (2006.01) C07K 1/02 (2006.01) C07K 1/08 (2006.01) C07K 5/02 (2006.01) C07K 5/06 (2006.01)

Patent

CA 2266757

There is provided a process for preparing a pharmacologically acceptable salt of N-(1(S)--ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid which comprises condensing an amino acid and N--(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanine- N-carboxy-anhydride under basic condition, carrying out decarboxylation under between neutral and acidic condition to obtain N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L- alanyl-amino acid, and forming a pharmacologically acceptable salt thereof, wherein the production of a by-product (3): (see formula 3) is suppressed by carrying out in an aqueous liquid a series of operations till formation of the pharmacologically acceptable salt or till isolation of the pharmacologically acceptable salt. The present invention enables to prepare the pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid having high quality, in a commercial scale with high yield and economical efficiency.

Divulgation d'un procédé de préparation d'un sel pharmaceutiquement acceptable d'un acide aminé N-(1(S)-éthoxycarbonyl-3-phénylpropyl)-L-alanylique comprenant les étapes suivantes : condensation d'un acide aminé et de N-(1(S)-éthoxycarbonyl-3-phénylpropyl)-L-alanine-N- carboxyanhydride dans des conditions basiques; décarboxylation du produit condensé dans des conditions de pH neutre à acide pour obtenir un acide aminé N-(1(S)-éthoxycarbonyl-3- phénylpropyl)-l-alanylique; formation d'un sel pharmaceutiquement acceptable au cours de laquelle la formation d'un sous-produit (3) est éliminée en réalisant en solution aqueuse une série d'opérations jusqu'à formation du sel pharmaceutiquement acceptable ou isolement de ce sel. La présente invention permet de préparer des sels pharmaceutiquement acceptables d'acides aminés N-(1(S)-éthoxycarbonyl-3-phénylpropyl)-l-alanyliques de haute qualité, à l'échelle commerciale avec un bon rendement et une bonne rentabilité.

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