Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
Suppression of Diketopiperazine Formation in Solid Phase Peptide Synthesis
KENJI SUZUKIKAZUO NITTANOBUYOSHI ENDO
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1975 Volume 23 Issue 1 Pages 222-224

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Abstract
When N-methylmorpholine salt of Boc-Ile was coupled with HCl·Pro-Pro-resin suspended in methylenechloride by dicyclohexylcarbodiimide, diketopiperazine formation of the dipeptide-resin was suppressed almost completely and the isoleucine residue in the synthesized Boc-Ile-Pro-Pro-resin was not racemized. Generalization of this coupling procedure in a schedule for solid phase peptide synthesis is suggested.
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© The Pharmaceutical Society of Japan
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