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作 者:苏荣 郭艳浩 蒿庆辉 郝思媛 段迎梅 张亚通[1] SU Rong;GUO Yan-hao;HAO Qing-hui;HAO Si-yuan;DUAN Ying-mei;ZHANG Ya-tong(College of Science,Hebei University of Science and Technology,Hebei Shijiazhuang 050000,China)
出 处:《广州化工》2024年第16期20-22,40,共4页GuangZhou Chemical Industry
摘 要:近年来,多肽类药物是国内和国际上新药研发的重点方向,并且多肽类药物研发也是国家重点支持发展的领域之一。多肽药物的研发的关键步骤是酰胺键的形成,而缩合剂是酰胺键形成的关键,现有的多肽类缩合试剂很多都有严重的弊端,像传统的多肽类缩合试剂会活化α类氨基酸而导致产物消旋化和其他副产物的生成,开发高效、副反应少的多肽缩合试剂尤为重要。本文综述了多肽合成中缩合试剂的研究进展,以便为多肽类药物的开发提供参考。In recent years,peptide drugs are the key direction of new drug research and development at home and abroad,and the research and development of peptide drugs is also one of the key areas supported by the state.The key step in the research and development of peptide drugs is the formation of amide bonds,and the condensation agent is the key to the formation of amide bonds.Many existing peptide condensation reagents have serious drawbacks,such as traditional peptide condensation reagents.Activation ofα-amino acids leads to racemization of products and generation of other by-products.It is particularly important to develop peptide condensation reagents with high efficiency and few side reactions.The research progress on condensation reagents in peptide synthesis was reviewed,in order to provide reference for the development of peptide drugs.
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