| 氮端Fmoc保护11-脱氧甘草次酸二肽类衍生物的合成 |
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| 引用本文： | 王军,胡小丽,文伟河,杨雷雷,杨晶,朱玉亮.氮端Fmoc保护11-脱氧甘草次酸二肽类衍生物的合成[J].化学试剂,2012,34(5):473-475. |
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| 作者姓名： | 王军 胡小丽 文伟河 杨雷雷 杨晶 朱玉亮 |
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| 作者单位： | 1. 江苏警官学院公安科技系,江苏南京 210012;南京工业大学生物与制药工程学院,江苏南京 210009
2. 南京工业大学生物与制药工程学院,江苏南京,210009 |
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| 摘 要： | 为获得高药效甘草次酸衍生物,以甘草次酸为原料,经过克莱门森还原得到11-脱氧甘草次酸,所得产物经溴乙烷乙酯化制得11-脱氧甘草次酸-30-乙酯,之后在THF溶液(四氢呋喃)中与Fmoc-Met-OH(Fmoc保护的甲硫氨酸)在DCC/DMAP中耦合制得11-脱氧甘草次酸-30-乙酯-3-Fmoc保护甲硫氨酸,然后在V(CHCl2)∶V(二乙胺)=1∶1溶液中脱去Fmoc保护基得到11-脱氧甘草次酸-30-乙酯-3-甲硫氨酸,再在THF溶液中与Fmoc保护缬氨酸,甘氨酸,苯丙氨酸通过DCC/DMAP耦合得标题化合物,收率95%～98%。其结构经1HNMR和MS表征。
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| 关 键 词： | 甘草次酸 Fmoc保护氨基酸 酯化 酰胺化 |
Synthesis of N Fmoc protection dipeptide of 11-deoxygly-cyrrhetinic acid derivatives |
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| WANG Jun
,
HU Xiao-li
,
WEN Wei-he
,
YANG Lei-lei
,
YANG Jing
,
ZHU Yu-liang.Synthesis of N Fmoc protection dipeptide of 11-deoxygly-cyrrhetinic acid derivatives[J].Chemical Reagents,2012,34(5):473-475. |
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| Authors: | WANG Jun HU Xiao-li WEN Wei-he YANG Lei-lei YANG Jing ZHU Yu-liang |
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| Affiliation: | 1 (1.Department of Forensic Science,Jiangsu Police Institute,Nanjing 210012,China;2.College of Biotechnology and Pharmaceutical Engineering,Nanjing University of Technology,Nanjing 210009,China) |
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| Abstract: | In order to obtain better efficacy glycyrrhetinic derivatives,3-amino acid of glycyrrhetinic acid derivatives were synthesized from glycyrrhetinic acid via deoxidation of 11-carbonyl,ethylesterrification of 30-carboxylic acid,esterification of 3-hydroxyl using Fmoc protected methionine by DCC/DMAP coupling method in tetrahydrofuran and deprotection Fmoc in a mixture solvent of CH2Cl2/(C2H5)2NH(V/V,1∶1).The final products N Fmoc protection dipeptide of 11-deoxyglycyrrhetinic acid derivatives were obtained by Fmoc protected amino acid include valine,glycine,phenylalanine and 3-amino acid of glycyrrhetinic acid derivatives with DCC/DMAP coupling method in tetrahydrofuran in yields of 95%～98% and characterized by 1HNMR and MS. |
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| Keywords: | glycyrrhetinic Fmoc protected amino acids esterification amidation |
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