- SYNTHESIS OF ENKEPHALINS BY THE METHOD OF POLYMERIC ACTIVATED ESTERS BASED ON 4-HYDROXY-3-NITROBENZOPHENONE
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Leucine- and methionine-enkephalins have been synthesized by the successive growth of the peptide chain from the C-end by the method of polymeric activated esters based on 4-hydroxy-3-nitrobenzophenone with yields of 90 and 70percent, respectively, calculated on the initial C-terminal amino acid.Polystyrene with 2percent of divinylbenzene was used as the polymeric matrix.Using the synthesis of methionine-enkephalin as an example, the possibility has been shown of using polymeric activated esters for the synthesis of peptides with a free carboxy group.
- Grigor'ev, E. I.,Chernova, S. V.
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p. 468 - 474
(2007/10/02)
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- AMINO ACIDS AND PEPTIDES. VIII. A WATER - SOLUBLE ACTIVE ESTER, PHENOLSULFONIC ACID DERIVATIVE
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N-protected amino acid 4-phenolsulfonic acid derivative esters, such as 2,6-dibromo-4-sulfophenyl ester sodium salt, 2,6-dichloro-4-sulfophenyl ester potassium salt and 2-nitro-4-sulfophenyl ester sodium salt, were prepared.These esters are water - soluble active esters, and were applied for rhe synthesys of Leu-enkephalin.Keywords - water - soluble active ester; 2,6-dichloro-4-sulfophenyl ester; 2,6-dibromo-4-sulfophenyl ester; 2-nitro-4-sulfophenyl ester; peptide synthesis; Leu-enkephalin
- Kawasaki, Koichi,Tsuji, Toshiki,Maeda, Misuko,Matsumoto, Tatsuya,Hirase, Katsuhiko
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p. 1044 - 1048
(2007/10/02)
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- AMINO ACIDS AND PEPTIDES. VII. PREPARATION AND APPLICATION OF A WATER-SOLUBLE ACTIVE ESTER, p-TRIMETHYLAMMONIOPHENYL ESTER
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A water-soluble active ester, p-trimethylammoniophenyl ester iodide, and its nitro derivative were prepared from N-procteted amino acid and the corresponding phenol derivative by the dicyclohexylcarbodiimide method.The synthetic esters were applied to the synthesis of Leuenkephalin.Keywords--water-soluble active ester; p-trimethylammoniophenyl ester iodide; Leuenkephalin; peptide synthesis
- Tsuji, Toshiki,Okusada, Satoshi,Maeda, Mitsuko,Kawasaki, Koichi
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p. 2214 - 2217
(2007/10/02)
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