Studies on the Use of Trityl Group in Peptide Synthesis

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  • トリチル基を保護基とするペプチド合成に関する研究
  • トリチルキ オ ホゴキ ト スル ペプチド ゴウセイ ニ カンスル ケンキュウ

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An industrial method for the synthesis of peptides using a trityl group as the protecting group has been investigated.<BR>The derivatives of the amino acids, containing a liophilic group in their side chain, such as γ-methyl, ethyl and benzyl glutamate, β-methyl, ethyl and benzyl aspartate and S-trityl cystein, were N-tritylated directly in good yields with 2-equiv. of trityl chloride in aprotic solvents in the presence of triethyl amine. In these reactions, it was found that the α-carboxyl group of amino acids derivatives was simultaneously tritylated during the N-tritylating process.<BR>Using these trityl derivatives, glutathione (GSH), α-aminobenzyl penicilline (ABP) and aspartyl phenylalanine methyl ester (APAM) were prepared in good yields.

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