Acta Chimica Sinica ›› 2001, Vol. 59 ›› Issue (10): 1740-1744. Previous Articles     Next Articles

Original Articles

HOBt, HOOBt, HOSu与惰性氯代烷溶剂之间的反应及其对 多肽合成影响的研究

纪建国;张德仪;江军;叶蕴华;邢其毅   

  1. 北京大学化学与工程学院;北京大学生命有机与分子工程教育部重点实验室
  • 发布日期:2001-10-15

Studies on the reaction of HOBt, HOOBt, and HOSu with chloroalkane solvents and their affects on the peptide synthesis

Ji Jianguo;Zhang Deyi;Jiang Jun;Ye Yunhua;Xing Qiyi   

  • Published:2001-10-15

HOBt, HOSu and HOOBt are the widely used reagents in the peptide synthesis, they are used as the activitor of carboxyl group and the inhibitor of racemization. HOBt, HOSu and HOOBt were found for the first time that they could react whith chloroalkane solvents in the presence of different base. The yields were realted to the reaction condition such as the quantity and variety of bases, reaction temperature and the structure of the reactants. The more of the bases used, the higher of the yield and reacton speed. HOBt is more active than HOSu, CH2Cl2 is easy to form disubstituted proucts, ClCH2CH2Cl is easy to form monosubstituted products. All of the products were purified by chromatography on silica-gel, eight new compounds were identified by MS and 1^H NMR. In the model synthesis of dipeptide BocAlaPheOCH3, the by-product was detected and the yield of the dipeptide was over 82%。

Key words: TRIAZINE P, CHLOROHYDROCARBON, POLYPEPTIDE, SOLVENTS

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