Synthesis of cyclic peptides
OwnerJun Liu, Xuedong Dai +1inventors
InventorsJun Liu, Xuedong Dai, Zhuang Su
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Abstract
The cyclic pentapeptide cyclo(-Arg-Gly-Asp-D-Phe-Lys-) is a highly potent and selective inhibitor for the αvβ3 integrin. A related compound, cyclo(-Arg-Gly-Asp-D-Phe-Val-), is a promising anticancer drug candidate; it has been found to inhibit angiogenesis and induce apoptosis in vascular cells. We have developed a synthesis of arginine containing cyclic peptides using the cyclizcation reagent 1-propanephosphonic acid cyclic anhydride (T3P) and the guanidine protecting group, 2,2,5,7,8-pentamethylchroman-6-sulfonyl (Pbf). This improved synthesis is environmentally friendly and is generally applicable to the synthesis of other cyclic peptides.
Claims12
A method of synthesizing cyclic peptides, the method comprising steps of:
- providing a linear peptide;
- and
- cyclizing the linear peptide.
A method of synthesizing cyclic peptides, the method comprising steps of:
- providing an arginine containing peptide wherein the arginine side chain is protected with 2,2,5,7,8-pentamethylchroman-6-sulfonyl (Pbf);
- and
- cyclizing the peptide using 1-propanephosphonic acid cyclic anhydride (T3P).
Dependencies are inferred from the claim text.