微波辅助固相合成苄基保护的天冬氨酸六肽

Solid-phase synthesis of protected Asp6 by microwave irradiation

目的固相合成天冬氨酸六肽。方法以Fmoc-Asp(OB zl)-OH为原料,苯并三氮唑-N,N,N,′N′-四甲基脲六氟磷酸酯为缩合剂,微波辅助逐步接肽法固相合成,三氟醋酸切割产物肽,纯化得保护的天冬氨酸六肽。结果产物结构经1HNMR,MS确证。结论微波法可以显著缩短固相合成反应的时间,提高产率。

OBJECTIVE To synthesis Asp6 by solid-phase method.METHODS Fmoc-Asp（OBzl）-OH was applied as the raw material,and o-Benzotriazol-1-yl-N,N,N′,N′-tetramethyluronium hexafluorophosphate as the coupling reagent.The protected Asp6 was synthesized on resin gradually by microwave irradiation,clearaged by trifluoroacetic acid,and purified.RESULTS Chemical structure of product was confirmed by 1HNMR and MS.CONCLUSION Microwave method can significantly shorten the time of solid-phase reaction and increase the yield.