Acetic Acid-Catalyzed Diketopiperazine Synthesis

Optically pure diketopiperazines were obtained in good yields when dipeptide esters were refluxed in 2-butanol containing 0.1 M acetic acid for 3 hours. When prolyl-amino acid ester was used as the starting material, 1 to 2 M acetic acid was the most effective concentration.

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Bibliographic Details
Published inChemical & pharmaceutical bulletin Vol. 29; no. 1; pp. 233 - 237
Main Authors MIHARA, YUICHI, ENDO, NOBUYOSHI, SUZUKI, KENJI, SASAKI, YUSUKE
Format Journal Article
LanguageEnglish
Published Tokyo The Pharmaceutical Society of Japan 01.01.1981
Japan Science and Technology Agency
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ISSN0009-2363
1347-5223
DOI10.1248/cpb.29.233

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Summary:Optically pure diketopiperazines were obtained in good yields when dipeptide esters were refluxed in 2-butanol containing 0.1 M acetic acid for 3 hours. When prolyl-amino acid ester was used as the starting material, 1 to 2 M acetic acid was the most effective concentration.
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ISSN:0009-2363
1347-5223
DOI:10.1248/cpb.29.233