丙氨瑞林的合成

Synthesis of Alarelin

以多肽固液组合合成方式,通过采用CTC树脂作为载体,HBTU作为缩合剂,HOSu或HOBt为活化剂,DIEA为有机碱,哌嗪为脱帽试剂逐步合成丙氨瑞林粗品(Pglu-His-Trp-Ser-Tyr-D-Ala-Leu-Arg-Pro-NHEt)。目标产物经液相色谱及质谱表征,该丙氨瑞林粗品产物产率为86.3%,纯度为91%。改进后的制备工艺以哌嗪作为脱帽试剂用CTC树脂合成片段,结合液相法合成丙氨瑞林适合大规模工业化生产,没有剧烈的化学反应;降低了生产成本。

Using polypeptide solid-liquid combination synthesis method,by using CTC resin as the carrier,HBTU as the condensing agent,HOSu or HOBt as the activator,DIEA as the organic base,and piperazine as the decapping reagent,the crude alarelin(Pglu-His-Trp-Ser-Tyr-D-Ala-Leu-Arg-Pro-NHEt)was synthesized.The target product was characterized by liquid chromatography and mass spectrometry.The yield of the crude alarelin product was 86.3%and the purity was 91%.The improved preparation process used piperazine as a decapping reagent to synthesize fragments with CTC resin,combined with the liquid phase method to synthesize alanorrelin,which was suitable for large-scale industrial production without severe chemical reactions,it reduced production costs.