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AssigneeKaneka Corporation
InventorsYasuyoshi Ueda, Koichi Kinoshita, Tadashi Moroshima, Yoshifumi Yanagida, Yoshihide Fuse
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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-carboxyanhydride 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): 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.
A process for preparing N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-L-proline maleate wherein a process in which steps for forming and crystallizing a salt in an aqueous liquid containing N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-L-proline and maleic acid are carried out in an aqueous liquid essentially consisting of water, is carried out in the coexistence of an inorganic salt and/or at from 40 to 70° C.
A process for preparing a pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid represented by a formula (2):
A process for separating N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-L-proline wherein, by separating a two-phase medium comprising water and an organic solvent having a low miscibility with water which medium contains N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-L-proline, at a temperature of at least 20° C., N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-L-proline is transferred into the organic solvent phase or, by separating the two-phase medium at a temperature of less than 20° C., N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-L-proline is transferred into the water phase.
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