关键词: 羟基苯并三氮唑, 三嗪P, 羟基琥珀酰亚胺, 氯代烃, 多肽, 溶剂

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