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