| 摘要 |
NEW MATERIAL:A compound shown by the formula I [R<1> is group shown by the formula VIII (R<3> and R<4> are OH, cyano, halogen, alkyl, etc.; m is 0-4; n is 0-3; A is SO2, or CO), etc.; R<2> is group shown by the formula IX (R<14> and R<15> are as shown for R<3>; f is 0-4; g is 0-3; D is -O-, -S-, etc.), etc.] and its acid addition salt acceptable as a drug. EXAMPLE:1-[N<2>-(7-Methoxy-2-naphthalenesulfonyl)-L-arginyl]-4-phenylp iperidine. USE:A preventive and remedy for pancreatitis. Having an inhibitory action with high specificity on trypsin. PREPARATION:A compound shown by the formula II is reacted with a compound shown by the formula III to give a compound shown by the formula IV (G' is guanidino- protecting group; G'' is alpha-amino-protecting group), alpha-amino-protecting group is eliminated by acidolysis, etc. to give a compound shown by the formula V, which is condensed with a compond shown by the formula VI (X is halogen), and subjected to hydrogenolysis, to give a compound shown by the formula I . |
