| 摘要 |
NEW MATERIAL:A compound shown by the formula I [R<1> is H, alkali metal atom, alkyl, benzyl, etc; R<2> is alkyl or benzyl; R<3> is H or methyl; R<4> is alkyl, phenyl, benzyl, phenetyl, the formula II (R<5> is alkyl may be replaced by OH, etc., or H; R<6> is H, alkoxy, etc.), R3 and R4 together with linked N form heterocyclic ring]. EXAMPLE:N-[ N'-( DL-3-trans-ethoxycarbonyloxirane-2-carbonyl )-L-leucyl ]cyclohexylamine. USE:An activity inhibitor of protease wherein thiol group takes part in the development of activity. PROCESS:A compound shown by the formula III (R<7> is H or alkali metal atom) is reacted with a halogenating agent to form an acid chloride, which is added to a solution having both a compound shown by the formula IV and a base (e.g., triethylamine) while the solution being cooled with ice and stirred to give a compound shown by the formula I. |
