| 摘要 |
<p>NEW MATERIAL:A compound of formulaI(R1, R2 are H, lower alkyl). EXAMPLE:L-Tylosyl-D-methioninesulfoxide-glycil-N-methylphenethylamine. USE:It is used as a medicine such as an analgesic. It has an antiagonistic activity against the opiate receptor. PREPARATION:The reaction of a dipeptide of formula II (A1 is amino-protecting group; A2 is H, hydroxyl protecting group) or its reactive derivative at the carboxyl group such as acid azide, mixed acid anhydride or active ester, with glycylamide derivative gives a compound of formula IV. Then, protecting groups are removed from the product to give the compound of formulaI. The reaction is usually carried out in a solvent such as THF, DMF or chloroform in a temperature range from about -20 deg.C to about 50 deg.C.</p> |
