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Synthesis of [D-Ala2]Leu-enkephalin and [D-Ala2, D-Leu5]Leu-enkephalin with high specific tritiated activity in the leucine residue

✍ Scribed by Hasegawa, Hiroshi; Shinohara, Yoshihiko; Baba, Shigeo


Book ID
121458571
Publisher
Royal Society of Chemistry
Year
1990
Weight
446 KB
Volume
10
Category
Article
ISSN
1472-7781

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D-Ma2, D-Leu51Enkephalin (DADLE) labelled with tritium in the 2,6-positions of N-terminus tyrosine residue has been prepared. Synthesis of the precursor peptide, [2,6-dibromo-Tyrl]DADLE, was performed by solid phase synthesis using F'moc strategy. The peptide was tritiated catalytically to yield [2

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Boc-Tyr-D-Ala-Gly was prepared by catalytic tritiation of protected, iodinated tripeptide. The protected tritiated tripeptide and the Phe-Leu-CH2C1 dipeptide were condensed by the mixed anhydride method. The p r o - 3 " tecting group was removed by HC1-methanol. The /JH/-DALECK had a specific activi