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目的:采用新的固相方法合成黑皮素环状类似物。方法:选用MBHA树脂和Fmoc/t-Butyl策略完成所有氨基酸缩合,利用4 mol.L-1HCl/Dioxane对成环的氨基酸Asp(OtBu)和Lys(Boc)侧链保护基进行脱除,在缩合剂作用下,裸露的氨基和羧基偶联成环。结果:利用此法成功地合成了MT-II及其三个全新的环肽类似物。结论:该方法操作简单,成本低;得到的产品纯度较高,易于纯化。
OBJECTIVE: To synthesize melanocortin cyclic analogs by a new solid-phase method. Methods: MBHA resin and Fmoc / t-Butyl strategy were used to complete all amino acid condensation. The cyclized amino acids Asp (OtBu) and Lys (Boc) side chain protecting groups were removed by 4 mol·L-1 HCl / A mixture of role, the naked amino and carboxyl coupling ring. Results: MT-II and its three new cyclic peptide analogs were successfully synthesized by this method. Conclusion: The method is easy to operate and has low cost. The obtained product has high purity and is easy to be purified.