| 摘要 |
1,182,450. Process for amino acids and peptides. FARBWERKE HOECHST A.G. 29 Aug., 1967 [27 Aug., 1966; 10 Feb., 1967], No. 39507/67. Heading C2C. In a process for preparing amino acids and polypeptides, an amino acid or polypeptide containing N-formyl groups or derivatives thereof, with the exception of esters with primary or secondary alcohols, are reacted with an at least equimolar amount of a compound R-NH-R<SP>1</SP> in which R is H, alkyl, optionally substituted aralkyl or aryl, alkanoyl, aroyl, alkyl or aralkyl-oxycarbonyl, carbamoyl or thiocarbamoyl or amidino, and R<SP>1</SP> is amino, or (when R is alkyl or aryl), alkylamino or arylamino, or (when R is H), OH or alkoxy or phenyl optionally substituted by alkyl, OH, alkoxy, amino and halogen and when R is H, alkyl or aralkyl and R<SP>1</SP> is amino or alkylamino the reaction is carried out in the presence of a weak organic acid. The following intermediates are prepared: BOC - Sa - Tyr - Sa - Met - Glu(OtBu) - - His - Phe - Arg - Try - Gly - Lys(For) - Pro - Val - Gly - Lys(For) - Lys(For) - Arg - Arg - Pro - Val - Lys (For)- Val-Tyr NH 2 (from the decapeptide and the tridecapeptide); H - Tyr - Ser - Met - Glu(OtBu)- His - Phe - Arg - Try - Gly - OH (from the BOC-blocked peptide) and For-Tyr-Ser-Met- Glu(OtBu) - His - Phe - Arg - Try - Gly - OH; Ac - Ser - Tyr - Ser - Met - Glu(OtBu) - His - Phe - Arg - Try - Gly - Lys(For) - Pro - Val - NH 2 (from the decapeptide and the tripeptide) and Ac - Ser - Tyr - Ser - Met - Glu(OH) - His- Phe - Arg - Try - Gly - Lys(For) - Pro - Val-NH 2 and BOC - D - Ser - Tyr - Ser - Met - Glu(OtBu)- His-Phe-Arg-Try-Gly-OH. |
