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Abstract <p>(2<i>S</i>,4<i>S</i>)-4-Amino-1-aryl-5-oxoprolines were synthesized by nucleophilic substitution of the bromine atom in dimethyl (2<i>S</i>,4<i>RS</i>)-4-bromo-<i>N</i>-phthaloylglutamate under the action of difluorosubstituted anilines followed by isolation of (2<i>S</i>,4<i>S</i>)-diastereomers and removal of protecting groups; subsequent coupling of their methyl esters with <i>N</i>-(purin-6-yl)-6-aminohexanoic acid and saponification of ester groups led to the formation of target conjugates. The saponification of ester groups was accompanied by minor epimerization.</p>

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Synthesis of Conjugates of N-(Purin-6-yl)-6-aminohexanoic Acid with 4-Amino-1-aryl-5-oxoprolines

  • 期刊论文

  • 发表日期：

    2025年6月1日

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  • A. Yu. Vigorov,
  • O. A. Vozdvizhenskaya,
  • A. A. Tumashov,
  • T. V. Matveeva,
  • I. N. Ganebnykh,
  • G. L. Levit,
  • V. P. Krasnov

摘要

Abstract

(2S,4S)-4-Amino-1-aryl-5-oxoprolines were synthesized by nucleophilic substitution of the bromine atom in dimethyl (2S,4RS)-4-bromo-N-phthaloylglutamate under the action of difluorosubstituted anilines followed by isolation of (2S,4S)-diastereomers and removal of protecting groups; subsequent coupling of their methyl esters with N-(purin-6-yl)-6-aminohexanoic acid and saponification of ester groups led to the formation of target conjugates. The saponification of ester groups was accompanied by minor epimerization.