トリチル基を保護基とするペプチド合成に関する研究

玉置 健太郎, 工藤 士郎

doi:10.5059/yukigoseikyokaishi.29.599

トリチル基を保護基とするペプチド合成に関する研究

DOI Web Site

玉置健太郎

協和醗酵工業株式会社堺工場
工藤士郎

協和醗酵工業株式会社

書誌事項

タイトル別名

Studies on the Use of Trityl Group in Peptide Synthesis
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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説明

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.