Synthesis of peptide amides by means of a solid phase method usi

Details Synthesis of peptide amides by means of a solid phase method usi Synthesis of peptide amides by means of a solid phase method usi

1988-04-06

1990-05-01

Reamer, James H.

Organic compounds -- part of the class 532-570 series

Organic compounds

Carboxylic acids and salts thereof

562460, 562468, 560 42, 560 57, 560 52, 530337, C07C10130

Patent

active

049220152

ABSTRACT:
The invention relates to new compounds of the formula ##STR1## in which R.sup.1 denotes (C.sub.1 -C.sub.8)-alkyl or optionally substituted (C.sub.6 -C.sub.14)-aryl, R.sup.2 denotes hydrogen or an amino acid residue which is protected by an amino protective group which can be cleaved off with weak acid or base, R.sup.3 denotes hydrogen or (C.sub.1 -C.sub.4)-alkyl, and Y.sup.1 -Y.sup.9 denote identical or different radicals hydrogen, (C.sub.1 -C.sub.4)-alkyl, (C.sub.1 -C.sub.4)-alkoxy or -O-(CH.sub.2).sub.n -COOH (with n=1 to 6), one of these radicals being -O-(CH.sub.2).sub.n -COOH. A process for the preparation thereof and the synthesis of peptide amides by means of a solid phase method using these new compounds (spacers) are described.

REFERENCES:
patent: 3825507 (1974-07-01), Boyd et al.
J. P. Tam et al, Tetrahedron Lett., vol. 22, pp. 2851-2854, (1981).
C. Ressler et al, J. Am. Chem. Soc., vol. 76, pp. 3107-3109 (1954).

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