| 摘要 |
1,268,463. Process for preparing peptides. ELI LILLY & CO. 5 May, 1970 [5 May, 1969], No. 21649/70. Heading C2C. Peptides are prepared by (a) admixing at least a 1.5 molar equivalent of an anhydride or mixed anhydride of an N-protected amino acid with one molar equivalent of a reactive basic C-protected peptide or amino acid in a non-aqueous, watermiscible solvent at between ambient room temperature and the freezing point of the reaction mixture for a time sufficient to allow complete reaction of the basic peptide; (b) hydrolysing the excess acid anhydride by contacting the reaction mixture with an aqueous buffer solution and (c) separating the peptide therefrom. Peptides prepared in the examples are CBO- ala - glu(N<SP>6</SP> - xanthyl) - OMe; CBO - arg(NO 2 )- ala - glu(N<SP>5</SP> - xanthyl) - OMe; CBO - leu - asp- (otBu) - OEt; CBO - tyr(tBu) - leu - asp(OtBu)- OEt; BOC - lys(CBO) - tyr(tBu) - leu - asp- (OtBu) - OEt; CBO - ser(tBu) - lys(BOC) - tyr- (tBu) - leu - asp(OtBu) - OEt; H-phe - phe- OMe; CBO - glu - asp(OtBu) 2 ; CBO - glu - asp- (OtBu) - OEt; CBO - ala - glu - asp(OtBu) 2 ; CBO - ala - glu - asp(OtBu)OEt; CBO - arg- (NO 2 ) - ala - glu - asp(OtBu) 2 ; CBO - arg(NO 2 )- ala - glu - asp(OtBu) - OEt; CBO - arg(CBO) 2 - ala - glu - asp(OtBu) 2 ; CBO - arg(CBO) 2 - arg- (acetyl) - ala - glu - asp(OtBu) 2 ; CBO - ser(tBu)- arg(acetyl) - arg(acetyl) - ala - glu - asp(OtBu) 2 ; CBO - glu - gly - OEt; CBO - ser(tBu) - glu - gly- OEt; CBO - try - leu - OMe; CBO - glu - tryleu - OMe; CBO - val - glu - try - leu - OMe; CBO - phe - val - glu - try - leu - OMe; BOC- phe - val - glu - try - leu - OMe; CBO - ser(tBu)- asp(OtBn) - OEt; CBO - thr(tBu) - ser(tBu)- asp(OtBu) - OEt; CBO - phe - thr(tBu) - ser- (tBu) - asp(OtBu) - OEt; and CBO - thr(tBu)- phe - thr(tBu) - ser(tBu) - asp(OtBu) - OEt. |
