利用脂溶性硅基载体连续流动液相合成维洛斯肽OA北大核心CSTPCD
Continuous Flow Liquid-phase Vialox Peptide Synthesis Using Hydrophobic Silyl Tag
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.
刘豪;刘冬梅;孙浩田;夏超;苏贤斌
青岛科技大学化工学院,青岛 266042南京工业大学化工学院,南京 210009
化学
脂溶性硅基载体连续流动液相多肽合成
Hydrophobic silyl tagContinuous flowLiquid-phase peptide synthesis
《高等学校化学学报》 2024 (007)
92-100 / 9
省部共建生态化工协同创新中心人才基金(批准号:1203042904001419)资助.Supported by the Talents Fund of the Provincial and Provincial Cooperative Innovation Center for Ecological Chemical Industry,China(No.1203042904001419).
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