| 摘要 |
1374379 Peptide synthesis TAKEDA YAKUHIN KOGYO KK 14 March 1973 [14 March 1972 21 March 1972 (2)] 12224/73 Heading C2C Peptide compounds are prepared by reaction, in the presence of a carbodiimide, of an amino acid, peptide, or an amino acid or peptide derivative in which at least one amino or imino group is protected with an N-hydroxy-norbornene dicarboximide to give an N-hydroxynorbornene dicarboximide ester I, and reaction of the compound I with a further amino acid, peptide or amino acid or peptide derivative having at least one unprotected amino or imino group. The compounds I are claimed per se. Intermediates isolated and peptides prepared are: N - hydroxy - 5 - norbornene - 2,3 - dicarboximide, Z - Pyroglu - ONBI (NBI is N - hydroxy - 5 - norbornene - 2,3 - dicarboximide ester); Z - Glu(OtBu) - ONBI; ZPyroglu - Glu(OBz) - OH; Z - Ala - NH 2 ; Z - Ala - Gly - OBz; Z - Val - Val - OBz; ZGly - Phe - Gly - OEt; Z - Gly - Phe - OH; ZPhe-Ile-OH; Z-Phe-Ile-Gly-OBz; Z-Glu- Ala - OBz; Z - Asn - Gly - OEt; Z- or HPyroglu - Glu - Ala - NH 2 ; Z - Pyroglu - His- OH; Z- or H - Pyroglu - His - Pro - NH 2 ; #(1-24)corticotropin; Z - Pyroglu - His - Trp- OBz; H - Pyroglu - His - Trp - Ser - Tyr - Gly- OtBu; Z - Arg(NO 2 ) - Pro - Gly - NH 2 ; ZLeu - Arg(NO 2 ) - Pro - Gly - NH 2 ; Z-Lys(IBOC)- Pro - Gly - NH 2 (IBOC = isobornyloxycarbonyl); Z - Leu - Lys(IBOC) - Pro - Gly - NH 2 ; BOCLeu - Orn(Z) - Pro - Gly - NH 2 ; H - Pyroglu- His - Trp - Ser - Tyr - Gly - Leu - Arg - Pro- Gly - NH 2 ; H - Pyroglu - His - Trp - Ser - Tyr- Gly - Leu - Lys - Pro - Gly - NH 2 ; H - Pyroglu- His - Trp - Ser - Tyr - Gly - Leu - Orn - Pro- Gly - NH 2 ; IBOC - Gly - Arg(NO 2 ) - Pro - Gly- NH 2 ; Z - Phe - Arg(NO 2 ) - Pro - Gly - NH 2 ; ZAla - Arg(NO 2 ) - Pro - Gly - NH 2 ; IBOC - Val- Arg(NO 2 ) - Pro - Gly - NH 2 ; Z - Ile - Arg(NO 2 )- Pro - Gly - NH 2 ; H - Pyroglu - His - Trp - Ser- Tyr - Gly - Gly - Arg - Pro - Gly - NH 2 ; HPyroglu - His - Trp - Ser - Tyr - Gly - Phe - Arg- Pro - Gly - NH 2 ; H - Pyroglu - His - Trp - Ser- Tyr - Glu - Ala - Arg - Pro - Gly - NH 2 ; HPyroglu - His - Trp - Ser - Tyr - Gly - Val - Arg- Pro . Gly - NH 2 ; and H - Pyroglu - His - Trp- Ser - Tyr - Gly - Ile - Arg - Pro - Gly - NH 2 .
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