- Method for preparing lisinopril intermediate
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The invention provides a method for preparing a lisinopril intermediate. The method comprises the following steps: treating (R)-2-hydroxy-4-phenylbutyrate in an organic solvent in the presence of alkali by using sulfonyl chloride so as to obtain a sulfonate solution; and reacting with trifluoroacetyllysine salt in the solution prepared in the previous step, separating after the reaction is ended, thereby obtaining N2-[1-(S)-alkoxycarbonyl-3-phenylpropyl]-N6-trifluoroacetyl-L-lysine. The method for preparing the lisinopril intermediate, provided by the invention, is short in synthetic route, simple and convenient in operation, low in cost and suitable for industrialized production.
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Paragraph 0041; 0042
(2017/07/21)
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- METHOD FOR PURIFYING N2-(1(S)-ETHOXYCARBONYL-3-PHENYLPROPYL)-N6-TRIFLUOROACETYL-L-LYSINE
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A process for purifying N2-(1(S)-ethoxycarbonyl-3-phenylpropyl)-N6-trifluoroacetyl-L-lysine which comprises subjecting N2-(1(S)-ethoxycarbonyl-3-phenylpropyl)-N6-trifluoroacetyl-L-lysine contaminated with impurities to crystallization from a solvent comprising a water-soluble non-protic organic solvent, thereby removing the impurities into the mother liquor and giving crystals of N2-(1(S)-ethoxycarbonyl-3-phenylpropyl)-N6-trifluoroacetyl-L-lysine, according to which N2-(1(S)-ethoxycarbonyl-3-phenylpropyl)-N6-trifluoroacetyl-L-lysine having a high quality can be obtained in a high yield and a high productivity and which is suitable for practice on an industrial scale.
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- N2 -carboxy-3-phenylpropyl)-l-lysine derivative and process of producing lysinolpril using the compound
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An N2 -(1-substituted-3-phenylpropyl)-L-lysine derivative is disclosed and is represented by formula (I) STR1 wherein R1 represents an acyl type or urethane type protective group; R2 represents a hydrogen atom, an alkyl group, or an aralkyl group. X represents a cyano (CN) group or an aminocarbonyl (CONH2) group; and the mark * represents the (S) position to the asymmetric carbon atom.
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