| 摘要 |
<p>NEW MATERIAL:A compound shown by formula I (R is group shown by formula II or -Gly-NH2). EXAMPLE:A compound shown by formula III. USE:An analgesic, stronger than morphine hydrochloride, etc., showing prolonged analgesic activity, having low toxicity and low dependence and showing im proved activity even by oral administration. PREPARATION:For example, Boc-Phe-ONSu (Boc is t-butoxycarbonyl; ONSu is N-hydroxysuccinimide ester) is condensed with H-betaAla-OBzl.Tos (Tos is tosyl) in the presence of triethylamine, etc., in a solvent such as DMF, etc., to give a compound shown by formula IV, which is treated with a solution of hydrochloric acid-dioxane to remove a protecting group Boc. Then, the com pound is successively condensed with Boc-D-Arg(NO2)-OH and Boc-Tyr-OH by the same method to give a compound shown by formula V, which is decom posed with an acid such as trifluoroacetic acid, etc., in the presence of a cationic scavenger such as anisole, etc., and deprotected to give a compound as exempli fied.</p> |
