| 摘要 |
<p>NEW MATERIAL:A tripeptide alkylamide of formula I (R1 and R2 are H or lower alkyl; R3 and R4 are H or acetyl). EXAMPLE:L-Tyrosyl-D-methioninesulfoxide-glycyl-L-phenylalaninol. USE:An analgesic and anesthetic agent, having the agonistic activity in opiate receptors, useful as an anesthetic antagonistic agent, and characterized by low toxicity and long duration. PROCESS:A compound of formula II (A1 is a protecting group of the amino group; A2 is OH) is condensed with a compound of formula III (A3 is a protecting group of the carboxyl group) by the ordinary peptide bond forming reaction, and the resultant product is then oxidized to give a compound of formula IV. A compound of formula V is separately subjected to the reductive elimination reaction to give a compound of formua VI, which is then reacted with the compound of formula IV by the azide method to afford a compound formula VII. The protecting group is then removed to give the aimed compound of formula I (R3 is H).</p> |
