摘要
目的布舍瑞林合成工艺的优化。方法由2-Cl-CTC树酯出发合成布舍瑞林肽树脂,再经裂解、乙胺化、催化氢化、选择性脱去-Trt保护基,得到布舍瑞林。结果布舍瑞林粗肽纯度为82%。经半制备型高效液相纯化后,纯度达98%以上,总收率为37%。结论经过优化缩短了反应时间,降低了合成成本,可为工业化生产提供借鉴。
Objective To optimize the synthesis process of buserelin. Methods Using 2-CI-CTC resin synthesis of buserelin peptide resin, then by cleavage, ethylamine, hydrogenation, selective removal of the -Trt protecting group, separation and purification, synthesis of bushruilin. Results The purity of the crude peptide was more than 82%. After the purification by semi-preparative RP-HPLC, the purity was more than 98%, and the overall yield was 37%. Conclusion The process optimization can shorten reaction time, reduce the synthesis cost, which may be useful for the industrial production.
出处
《中国抗生素杂志》
CAS
CSCD
北大核心
2016年第4期285-288,共4页
Chinese Journal of Antibiotics
基金
河北省海外高层次人才"百人计划"资助项目(No.E201200002)
关键词
布舍瑞林
固相合成
工艺优化
Bushruilin
Solid phase synthesis
Process optimization
