Cyclization of peptides

Details Cyclization of peptides Cyclization of peptides

1976-07-28

1978-07-25

Phillips, Delbert R.

Chemistry of carbon compounds

Miscellaneous organic carbon compounds

C-metal

C07C10352

Patent

active

041028775

ABSTRACT:
The invention disclosed herein relates to the novel method for the preparation of cyclic peptides, wherein a linear peptide is reacted, in solution in a polar organic solvent, with an insoluble, resin-bound carboxyl-activating reagent such as resin-bound isopropylcarbodiimide. Cyclic peptides thus obtained have been found to retain biological activity characteristic of their linear counterparts, with increased biostability; the cyclic peptide, Gramicidin S, which can be prepared by this method, is a valuable antibacterial.

REFERENCES:
patent: 3705887 (1972-12-01), Wieland et al.
patent: 3719656 (1973-03-01), Jolles
patent: 3753970 (1973-08-01), Bouchaudon et al.
Ned M. Wernshenker, et al., Tet. Let. 32, pp. 3281-3284 (1972).
Von R. Schwyer, et al., Hel. Chim. Acta. 40, 1957, pp. 624-639.
Motonori Ohno, et al., J. Am. Chem. Soc. 93, 1971, pp. 5251-5254.

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