加压素固相合成方法的研究

Study on Solid-phase Synthesis of Vasopressin

建立了一个加压素固相合成的改良法,Boc-Gly挂树脂的方法由钾盐改为铯盐法,Cys的巯基用pMeBzl保护,其他氨基酸侧链均不保护,从而避免了钠/液氨处理。

An improved solid phase synthesis of vasopressin is described. The thiol groups of two Cys were protected by p methoxybenzyl, and all other functional groups on the side chain of amino acids were not protected. For loading the C terminal Gly on to the Merrifield resin, the cesium salt of Boc Gly OH was used instead of the potassium salt with over 99% yield of ester formation. The final protected peptide resin was treated with ammonia in methanol to get p methoxybenzyl protected nonapeptide amide. After removal of the two p methoxybenzyl groups with mercuric acetate, the two Cys at the position 1 and 6 of the product were oxidized by air to form disulfide bond.