摘要
采用Fmoc固相合成法合成血管紧张素Ⅱ,通过采用高替代度Fmoc-Phe-Wang树脂作为固相载体、FmocArg(Pbf)-OH/HBTU/HOBt/DIPEA与Fmoc-Arg(Pbf)-OH/HOBt/DIC并用偶联体系、三氟乙酸/三异丙基硅烷/水裂解体系等措施,提高了合成工艺的经济性、安全性、易操作性和生产效率,且所得产品粗品的纯度高达93.5%。
Solid-phase synthesis of angiotensin Ⅱ was performed by taking high degree of substitution Fmoc-Phe-Wang resin as a solid carrier, both Fmoc-Arg(Pbf)-OH/HBTU/HOBt/DIPEA and Fmoc-Arg(Pbf)-OH/HOBt/DIC as coupling system, trifluoroacetic acid/triisopropylsilane/water as hydrolysis system and other measures so as to improve the efficiency, safety and operability of the synthesis process and the production efficiency, and the purity of angiotensin Ⅱ crude product could reach to as high as 93.5%.
作者
江锡铭
黄龙
黄臻辉
JIANG Ximing;HUANG Long;HUANG Zhenhui(SPH No.1 Biochemical & Pharmaceutical Co., Ltd., Shanghai 200240, China)
出处
《上海医药》
CAS
2019年第7期69-70,73,共3页
Shanghai Medical & Pharmaceutical Journal
关键词
血管紧张素Ⅱ
固相合成
高替代度树脂
angiotensin Ⅱ
solid-phase synthesis
resin of high substitution