| 摘要 |
NEW MATERIAL:An epoxysuccinylamino acid derivative of formula I [R<1> is H, alkali metal, alkyl, alkenyl, alkynyl, II (B is alkylene; X is halogen, methyl); R<2> is amino, -O-R<3> (R<3> is H, alkali metal, alkyl, benzyl); A is (protected) amino, (protected) guanidyl, imodazole-substituted alkylene]. EXAMPLE:N<alpha>- ( DL-3-Benzyloxycarbonyloxirane-2-carbonyl-N<alpha> -carbobenzoxy-L- ornithine benzyl ester. USE:Agent for inhibiting the activity of proteinase wherein the activity is attributable to the thiol group. The compound is low-toxic, and does not accelerate the permeation of blood. PROCESS:The compound I is prepared, e.g. by converting the epoxysuccinic acid mono-ester of formula III (R<4> is H, alkali metal) to acid chloride, and reacting with an amino acid ester of formula IV. |
