布舍瑞林合成工艺的优化

Synthesis process optimization of buserelin

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.