| 摘要 |
<p>1,218,251. Protection of amino groups in peptide synthesis. CIBA Ltd. 22 Jan., 1968 [25 Jan., 1967; 28 Aug., 1967; 6 Dec., 1967], No. 3194/68. Heading C2C. A process for the temporary protection of amino groups in peptide synthesis by acylating the amino group and then eliminating the acyl group introduced uses the novel group in which R 1 is C 1-5 alkyl, R 2 C 1-5 alkyl or phenyl, and R 3 phenyl and in which the phenyl radicals may be substituted by C 1-5 alkyl, phenyl or C 7-11 alkylphenyl. Nα- acyl -α- amino acids, peptides and function derivatives in which the acyl group is as above, and compounds of the formula in which X is -NHNH 2 or -N 3 are claimed per se. Intermediates prepared are Nα- 2 - (p - diphenylyl) - isopropyloxy - carbonyl - lys(BOC)- lys(BOC) - OMe; N<SP>α</SP> - 2 - (p - diphenylyl)- isopropyloxy - carbonyl - pro - leu - glu(OtBu) Phe - OtBu; N<SP>a</SP> - 2 - (p - diphenylyl) - isopropyloxy - carbonyl - lys(BOC) - met - OMe; H- lys(BOC) - met - OMe; N<SP>a</SP> - 2 - (p - diphenylyl)- isopropyloxy - carbonyl - tyr - lys(BOC) - met- OMe; H-tyr - lys(BOC) - met - OMe; N<SP>α</SP> - 2- (p - diphenylyl) - isopropyloxy - carbonyl - protyr - lys(BOC) - met - OMe; H - Pro - tyr - lys- (BOC) - met - OMe; CBO - gly - glu - di - tBuester; N,S - di - trityl - L - cysteinyl - glycyl- L - glutamic acid - di - t - butyl - ester; S - trityl. L - cysteinyl - glycyl - L - glytamic acid - di - t- Butyl - ester; N<SP>a</SP> - 2 - (p - diphenylyl) - isopropyloxy - carbonyl - val - cys(S - trity) - glyglu(OtBu) 2 ; and N<SP>a</SP> - 2 - (p - dipehnylyl) - isopropyloxy - carbonyl - leu - val - cys(S . trityl)- gly - glu - (OtBu) 2 . Peptides prepared in the examples by use of the method of paragraph one are H - lys(BOC)- lys(BOC) - OMe; H - pro - leu - glu(OtBu). Phe - OtBu; CBO - phe - lys(BOC) - gly- NHNH 2 ; and H - pro - tyr - lys(BOC) - met- NHNH 2 .</p> |
