【摘要】 胰岛素B链N-端八肽衍生物,卽cb·phe·val·asp（NH₂）·glu（NH₂）·（im-Bz）his·leu·（S-Bz）cys·gly·OC₂H₅,曾用cbz·（im-Bz）his·leu·OH与H·（S-Bz）cys·gly·OC₂H₅借DCCI缩合生成cbz·（im-Bz）his·leu·（S-Bz）cys·gly·OC₂H₅,然后经溴化氢的冰醋酸溶液脱去苄氧羰基后,依次与cbz·glu（NH₂）·ONP,cbz·asp（NH₂）·ONP,cbz·val·ONP和cbz·phe·ONP缩合生成。此外,该八肽衍生物还曾用cbz·phe·val·ONP和B_3—8b缩合或cbz·phe·val·asp（NH₂）·N₃和B_4-8b缩合生成。所得八肽经溴化氢的冰醋酸溶液脱去苄氧羰基后,能为氨肽酶完全消化。更多还原

【Abstract】 Carbobenzoxyphenylalanylvalylasparaginylglutaminyl(N^im-benzyl)histidylleucyl（S-ben2yl）cysteinylglycine ethyl ester(B_1-8), a derivative of the N-terminal octapeptide of the Bchain of insulin, has been prepared by stepwise condensation starting from(N^im-benzyl)histidylleucyl（S-benzyl）cysteinylglycine ethyl ester(B_5-8b)with the p-nitrophenyl esters of carbobenzoxyglutamine, carbobenzoxyasparagine, carbobenzoxyvaline and carbobenzoxyphenylalanine respectively.(B_5-8b)was obtained by decarbobenzoxylation of carbobenzoxy(N^im-benzyl)histidylleucyl（S-benzyl）cysteinylglycine ethyl ester which was synthesized by coupling carbobenzoxy(N^im-benzyl)histidylleucine with（S-benzyl）cysteinylglycine ethyl ester through the carbodiimide method. Besides, the octapeptide derivative(B_1-8)has also been synthesized either by coupling the carbobenzoxyphenylalanylvaline p-nitrophenyl ester with asparaginylglutaminyl(N^im-benzyl)histidylleucyl（S-benzyl）cysteinylglycine ethyl ester or by condensing the carbobenzoxyphenylalanylvalylasparagine azide with glutaminyl(N^im-benzyl)histidylleucyl（S-benzyl）cysteinylglycine ethyl ester.The N^im,S-dibenzylated octapeptide ethyl ester, obtained by decarbobenzoxylation of B_1-8with hydrogen bromide in glacial acetic acid, could be completely digested by leucineaminopeptidase.更多还原