Acid-labile anchor groups for the synthesis of peptide...

Details Acid-labile anchor groups for the synthesis of peptide... Acid-labile anchor groups for the synthesis of peptide...

C - Chemistry, Metallurgy

07

K

260/468.1, 530/1

C07K 7/06 (2006.01) C07C 59/64 (2006.01) C07C 59/90 (2006.01) C07C 233/25 (2006.01) C07C 271/22 (2006.01) C07K 1/00 (2006.01) C07K 1/04 (2006.01)

Patent

CA 1341386

Acid-labile anchor groups for the synthesis of peptide amides by a solid-phase method The invention relates to new compounds of the formula (See formula I) in which R1 denotes (C1-C8)-alkyl, R2 denotes an amino acid residue which is protected with a urethane protective group which can be eliminated with weak acid or base, or denotes an amino protective group which can be eliminated with weak acid or base, R3 denotes hydrogen or (C1-C4)-alkyl, and Y1-Y9 denote identical or different radicals hydrogen, (C1-C4)-alkyl, (C1-C4)- alkoxy or -O-(CH2)n-COOH (with n - 1 to 6), with one of these radicals being -O-(CH2)n-COOH, or Y1, Y2 and Y5-Y9 denote identical or different radicals hydrogen, (C1-C4)-alkyl or (C1-C4)-alkoxy, Y3 denotes hydrogen or (C1-C8)-alkoxy and Y4 denotes -(CH2)n-COOH or -NH-CO-(CH2)n- COOH (with n = 1 to 6). Processes for the preparation thereof and the synthesis of peptide amides by a solid-phase method using these new compounds (spacers) are described.

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