利用脂溶性硅基载体连续流动液相合成维洛斯肽  

Continuous Flow Liquid-phase Vialox Peptide Synthesis Using Hydrophobic Silyl Tag

作　　者：刘豪 刘冬梅 孙浩田 夏超 苏贤斌 LIU Hao;LIU Dongmei;SUN Haotian;XIA Chao;SU Xianbin(College of Chemical Engineering,Qingdao University of Science and Technology,Qingdao 266042,China;College of Chemical Engineering,Nanjing Tech University,Nanjing 210009,China)

机构地区：[1]青岛科技大学化工学院,青岛266042 [2]南京工业大学化工学院,南京210009

出　　处：《高等学校化学学报》2024年第7期92-100,共9页Chemical Journal of Chinese Universities

基　　金：省部共建生态化工协同创新中心人才基金(批准号:1203042904001419)资助.

摘　　要：提出了一种新型脂溶性硅基载体4,4-二(叔丁基二苯基硅氧基)二苯甲胺(BPPM),可在微反应器中连续流动条件下快速液相合成多肽.所设计的连续流动装置由偶联单元(微通道反应器)、脱保护单元(填充床反应器)和水洗单元(微通道混合器)组成.该过程中使用绿色溶剂(以乙酸乙酯代替N,N-二甲基甲酰胺)和Cbz保护氨基酸(清洁的脱保护代替哌啶脱Fmoc保护),以环境友好的方式合成了高纯度(粗品>95%)的维洛斯肽,合成效率高(每偶联一个氨基酸<5 min).该研究成果易于工业化放大生产,为大规模绿色高效合成多肽提供了新方案.A novel hydrophobic silyl tag bis{4-[(tert-butyldiphenylsilyl)oxy]phenyl}methanamine(BPPM)was proposed for rapid liquid-phase peptide synthesis under continuous flow in a microreactor.The designed continuous flow device consists of a coupling unit(micro-channel reactor),a deprotection unit(packed-bed reactor)and a washing unit(micro-channel mixer).In this process,a green solvent(ethyl acetate instead of N,N-dimethylace-tamide)and Cbz-protected amino acids(clean deprotection instead of piperidine Fmoc-deprotection)were used.Vialox peptide with high purity(>95%crude)was synthesized in an environmentally friendly way,with high synthesis efficiency(each amino acid per coupling<5 min).The results are easy to scale up and provide a new strategy for large-scale green and efficient synthesis of peptides.

关 键 词：脂溶性硅基载体 连续流动 液相多肽合成 

分 类 号：O629.72[理学—有机化学]