| 摘要 |
NEW MATERIAL:A compound of formula I [R<3> is lower alkyloxycarbon, -CH2OH, formyl; R<1> is H, lower alkyl; R<2> is phenyl, formula II (R<4> is H, halogen, etc.; R<5> equals to R<1>; n is 0 or 1; A is 0, methylene, hydroxymethylene, phenyl- methylene or R<1> and R<2> incorporate to form aromatic ring benzylidene which may be substituted]. EXAMPLE:N-(3-Phenoxypropionyl)-prolinol. USE:Medicine. A proline endopeptidase inhibitor and antiamnnestic. PREPARATION:A carboxylic acid of formula III, a carboxylic chloride of formula IV or a carboxylic anhydride of formula V is subjected to condensation reaction with a proline of formula VI (R<6> is R<1>), its alkyl ester or their hydrochloride to give a compound of formula I where R<3> is lower alkyloxycarbonyl. The product is reduced to give a compound of formula I where R<3> is -CH<2>OH and the product is oxidized to give the third compound of formula I where R<3> is formyl.
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