Process for the low-racemization preparation of peptide intermediates of the synthesis of gonadorelin and gonadorelin analogs, and new intermediates for this process
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United States of America Patent
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Sep 1, 1987
Grant Date -
N/A
app pub date -
Mar 25, 1985
filing date -
Mar 27, 1984
priority date (Note) -
Expired
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Abstract
The invention relates to a process for the preparation of peptides of the formula I U--A.sup.1 --A.sup.2 13 A.sup.3 --A.sup.4 --A.sup.5 --X(I) in which U denotes a urethane protective group, A.sup.1 denotes Trp or D-Trp, A.sup.2 denotes Ser, Ala or Thr, A.sup.3 denotes Tyr or Phe, A.sup.4 denotes Gly, the residue of a D-amino acid or the residue of a D-amino acid derivative, A.sup.5 denotes Leu, N-methyl-Leu, N-ethyl-Leu, Ser(Bu.sup.t), Cys(But), Asp(OBu.sup.t), Glu(OBu.sup.t), Orn(Boc) or Lys(Boc) and X denotes OBu.sup.t or A.sup.6 --Pro--Y, where A.sup.6 represents Arg, Orn, Lys or homoarginine, and Y represents Gly--NH.sub.2, NH--NH--CO--NH.sub.2, (C.sub.1 -C.sub.3)-alkylamino, cyclopropylamino, (C.sub.1 -C.sub.3)-alkylamino which is substituted with hydroxyl or fluorine, or cycloalkylamino which is substituted with hydroxyl or fluorine, using tripeptides of the formula II, U--A.sup.1 --A.sup.2 --A.sup.3 --OH, in which the residues are defined as above. The invention also relates to peptides of the formula II as intermediates in this process.
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