| 新型黑皮素类似物的固相环肽合成 |
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| 引用本文： | 孙彭利,冯思良,刘克良. 新型黑皮素类似物的固相环肽合成[J]. 中国新药杂志, 2009, 18(2): 159-162 |
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| 作者姓名： | 孙彭利 冯思良 刘克良 |
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| 作者单位： | 军事医学科学院毒物药物研究所，北京100850 |
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| 摘 要： | 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-1 HCl/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。
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| 关 键 词： | MT-II；黑皮素；非天然氨基酸；环肽；固相合成 |
Solid-phase synthesis of new cyclic melanotropin analogues |
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| SUN Peng-li,FENG Si-liang,LIU Ke-liang. Solid-phase synthesis of new cyclic melanotropin analogues[J]. Chinese Journal of New Drugs, 2009, 18(2): 159-162 |
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| Authors: | SUN Peng-li FENG Si-liang LIU Ke-liang |
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| Affiliation: | InstitutionofPharmacologyandToxicology,AcademyofMilitaryMedicalScience,Beijing100850,China |
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| Abstract: | Objective: To prepare cyclic melanotropin analogues using a new solid-phase synthesis method. Methods: All the amino acids were step-wise assembled on MBHA resin by Fmoc/t-Butyl strategy, then remove the tBu and Boc from the Asp (OtBu) and Lys (Boc) using the 4 mol•L-1 HCl/Dioxane. The cyclization was finished through the coupling of the naked -NH2 and -COOH with condensing agent. Results: MT-II and its three novel cyclic analogues were successfully synthesized by the method. Conclusion: This method is easily handing with high yield and low cost for preparing cyclic peptides. |
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| Keywords: | MT-II melanocortin unnatural amino acid cyclic peptide solid-phase synthesis |
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