| 摘要: |
| 研究了Fmoc-Asn(Trt)-OH与Wang树脂的酯化反应工艺.探讨了反应策略、溶剂体系、投料比、反应时间以及反应温度等条件对手工合成Fmoc-Asn(Trt)-Wang树脂反应的影响.并用微波辅助方法与常规方法进行了对比.实验结果表明了采用HBTU/HOBt/DIEA方法的连接效率最高.对反应的优化结果为:NMP/DCM体积比为1∶7,体系、摩尔比为3∶1,每次反应时间4 h,温度40℃.微波对本酯化反应影响不大. |
| 关键词: 固相多肽合成(SPPS) Wang树脂 Fmoc-Asn(Trt)-OH 微波 |
| DOI： |
| 分类号:TQ32 |
| 基金项目: |
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| Synthesis of Fmoc -Asn (Trt) - Wang Resin |
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| Abstract: |
| The esterification process of Fmoc-Asn(Trt)-OH and Wang resin was studied by solid phase synthesis.The effects of reaction strategy,solution,molar ratio,reaction time and reaction temperature on the yield of Fmoc-Asn(Trt)-Wang resin were investigated and the results of microwave-assisted synthesis and manual synthesis were compared.The results indicated that the HBTU/HOBt/DIEA strategy was the best method and the optimum reaction conditions for the esterification were set at temperature 40℃,molar ratio 3:1,reaction time 4h using NMP/DCM(1:7,v/v) solution.The esterification process was hardly influenced by microwave radiation. |
| Key words: solid phase peptide synthesis Wang resin Fmoc-Asn(Trt)-OH microwave |
