Process for preparing peptide synthons

Chemistry: natural resins or derivatives; peptides or proteins; – Peptides of 3 to 100 amino acid residues – Synthesis of peptides

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530334, 530338, C07K 102, C07K 106

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active

050773879

ABSTRACT:
The present invention relates to a process for preparing peptide synthons in which the optical purity of each of the peptides to be condensed is retained.
According to this process, a silyl derivative of an amino acid or peptide, which is activated by a complex chloroimmonium salt, a complex coordinated phosphorus halide, oxyhalide salt or a complex oxalyl halide salt, is prepared. The activated peptide is then condensed with an N-silyl amino acid or peptide in which the acid group is protected.

REFERENCES:
patent: 4725645 (1988-02-01), Anteunis et al.
Fournier, A., et al., Int. J. Peptide Protein Res., 31:86-97, 1988.
Vanfleteren, L., et al., Bull. Soc. Chem. Belg., 97:505-517, 1988.
Tung, R., et al., J. Org. Chem., 51:3350-3354, 1986.
Kricheldorf, H., Liebigs Ann. Chem., 763:17-38, 1972.
Miyazawa et al., Peptide Chemistry, 1982, pp. 69-74.
Arnold et al., Synthetic Reactions of Dimethylformamide XIV., 1961.

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