精氨酸加压素 V2受体拮抗剂托伐普坦的合成进展

摘要

Heart failure is a common syndrome with a high mortality,although a speedy progress has been achieved in its mechanism and treatment in recent years. But its incidence rate and mortality rate are high. human arginine vasopressin is the main reason of the high mortality rate. FDA had approved Tolvaptan,a selective vasopressin — receptor antagonist that can be taken orally,for the treatment of patients with heart failure. In this article,we discussed the synthesis of tolvaptan and its intermediates,evaluate its merits and faults.%心力衰竭是一种常见的综合征，虽然它的发病机制和治疗研究迅速发展，但是发病率和死亡率都很高。精氨酸加压素是导致心力衰竭死亡率居高的原因之一。托伐普坦是2009年美国上市世界上首个口服精氨酸加压素 V2受体拮抗剂。本文综述了托伐普坦的合成方法及部分中间体的合成，并评价其优缺点。