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用液相法合成了ACTH4~10片段,并对7位氨基酸残基进行替换,获得2个类似物.从C端逐步接肽时,35mol/L氯化氢乙酸乙酯溶液可有效地脱去叔丁氧羰基保护基,偶联反应用DCC作缩合剂,合成2肽至4肽需Hobt活化,合成5肽至7肽若用Hobt活化可导致收率降低.该方法可用于类似片段的大量合成.
ACTH4 ~ 10 fragments were synthesized by liquid phase method, and the 7 amino acid residues were replaced to obtain two analogues. From the C-terminal peptide, 3 5mol / L hydrogen chloride ethyl acetate solution can effectively remove the tert-butoxycarbonyl protecting group coupling reaction using DCC as a condensing agent to synthesize peptide 2 to 4 peptides to be Hobt activation, The activation of Hobt with synthetic 5-peptide to 7-peptide results in a decrease in yield. This method can be used for mass synthesis of similar fragments.