Process for the deprotection of protected thiols

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

Reexamination Certificate

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C530S336000, C530S332000, C562S426000, C562S556000, C568S021000

Reexamination Certificate

active

06906171

ABSTRACT:
The synthesis of peptides comprising disulphide bridges is challenging since it is difficult to ensure that the correct cysteine residues combine to form the desired disulphide bridges. The present invention describes novel protection techniques useful in the preparation of peptides. Described is a process for the deprotection of an Acm-, MBzl- and/or tBu-protected thiol which comprises reacting said protected thiol with an acid in the presence of an oxidising agent at a temperature sufficient to effect deprotection and generation of disulphide bonds.

REFERENCES:
Koide et al. 1993. Chem. Pharm. Bull. vol. 41, No. 6, pp. 1030-1034.
Musiol et al. 1994. Biopolymers, Vo. 34, pp. 1553-1562.
Barany and Merrifield “The Peptides” vol. 2, Ed. Gross and Minehoffer, Academic Press, pp. 233-240 (1980).
Veber, et.al. in J. Am. Chem. Soc. 94, pp. 5456-5461 (1972).
Van Rietschoten, et.al. “Cysteine Protection in Solid Phase Synthesis of Apamin” pp. 522-524 (1977).
Singh, et.al. Tetrahedron Letters. vol. 37, No. 24, pp. 4117-4120 (1996).
Otaka, et.al. Tetrahedron Letters, vol. 32, No. 9 pp. 1223-1226 (1991).
Akaji, et.al. J. Am. Chem. Soc., vol. 114, No. 11, pp. 4137-4143 (1992).
Sieber, et.al. Helv. Chim Cata. 57 pp. 2617-2621 (1974).
Atherton, et.al. J. Chem. Soc. Perkin Trans. 1, p. 2065 (1985).
Akaji, et.al. J. Am. Chem. Soc. 115, p. 11384 (1993).
Hargittai, et.al., J. Peptide Res. 54, pp. 468-479 (1999).
Tam, et.al. J. Am. Chem Soc. 113, p. 6657-6662 (1991).
Cuthbertson, et.al. Tetrahedron Letters, 41 pp. 3661-3663 (2000).
Tamamura, et.al., Intl Journal of Peptide & Protein Research, 45, No. 4, pp. 312-319 (1995).

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