Process for the low-racemization preparation of peptide...

Details Process for the low-racemization preparation of peptide... Process for the low-racemization preparation of peptide...

C - Chemistry, Metallurgy

07

K

530/7.2

C07K 7/06 (2006.01) C07K 5/06 (2006.01) C07K 5/08 (2006.01) C07K 5/097 (2006.01) C07K 7/23 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1278650

Abstract of the Disclosure: The invention relates to a process for the prepa- ration of peptides of the formula I U - A1 - A2 - A3 - A4 - A5 - X (I) in which U denotes a urethane protective group, A1 denotes Trp or D-Trp, A2 denotes Ser, Ala or Thr, A denotes Tyr or Phe, A4 denotes Gly, the residue of a D-amino acid or the residue of a D-amino acid derivative, A5 denotes Leu, N-methyl-Leu, N-ethyl-Leu, Ser(But), Cys(But), Asp(OBut), Glu(OBut), Orn(Boc) or Lys(Boc) and X denotes OBut or A6-Pro-Y, where A6 represents Arg, Orn, Lys or homoarginine, and Y repre-sents Gly-NH2, NH-NH-CO-NH2, (C1-C3)- alkylamino, cyclopropylamino, (C1-C3)-alkylamino which is substituted with hydroxyl or fluorine, or cycloalkylamino which is substituted with hydroxyl or fluorine, using tripeptides of the formula II, U - A1 - A2 - A3 - OH, in which the residues are defined as above. The inven- tion also relates to peptides of the formula II as inter- mediates in this process.

477529

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