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布舍瑞林(Buserelin)是根据促性腺激素释放激素(GnRH)改造的多肽类药物。临床上主要用于乳腺癌、前列腺癌等疾病的治疗。该文主要对布舍瑞林合成方法进行研究:以DIC/HOBT为缩合剂,Boc合成法与Fmoc合成法联用的方法进行固相合成,乙胺/甲醇溶剂作为切割液,直接裂解树脂生成C端的乙胺基的方法合成布舍瑞林。并对合成的产物进行了结构鉴定。最终产品纯度为97%。该合成方法简单易行,产品纯度较高,适合用于布舍瑞林工艺开发。
Buserelin is a peptide based on gonadotropin-releasing hormone (GnRH). Clinically used mainly for breast cancer, prostate cancer and other diseases. In this paper, we mainly study the synthetic methods of buserelin: solid-phase synthesis with Boc synthesis and Fmoc synthesis using DIC / HOBT as condensing agent and ethylamine / methanol solvent as the cutting fluid to directly cleave the resin Buserelin was synthesized by a C-terminal ethylamino group. The structure of the synthesized product was identified. The final product has a purity of 97%. The synthesis method is simple and easy, and the purity of the product is high, which is suitable for the process of buserelin.