夏超,颜阳丽,黄玉龙,苏贤斌

• 1:南京工业大学化工学院

摘要(Abstract)：

针对传统环肽合成过程中存在的有毒溶剂（如二甲基甲酰胺（DMF）和二氯甲烷（DCM））使用、脱保护试剂（如哌啶）受控、环化效率低和对特定氨基酸（如Cys、Lys）依赖等问题，文中提出了一种绿色、高效的环肽合成策略。该策略基于新型可溶性硅基疏水标签（双（4-（（三异丙基硅烷基）氧基）苯基）甲基）肼（BTPH），结合连续流微反应技术，构建包含偶联、脱保护（四氢吡咯替代哌啶）及洗涤萃取三大模块的集成化系统，并采用低毒性乙酸乙酯（EA）替代DMF等传统有害溶剂。结果表明，该策略可高效合成线性Heterophyllin B肽酰肼，粗产物纯度>90%。此外，通过原位生成的酰基叠氮中间体在温和条件下完成环化，环化转化率较传统方法提升>30%，原子经济性提升，整体合成成本降低约60%。研究结论为绿色连续流合成天然环肽提供了可行路径，对复杂多肽的模块化制备具有重要参考价值。

关键词(KeyWords)： 可溶性标签;Heterophyllin B;连续流动;微通道反应器

Abstract:

Keywords:

基金项目(Foundation): 江苏高校优势学科建设工程资助项目（PAPD）

作者(Author): 夏超,颜阳丽,黄玉龙,苏贤斌

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