一种磺达肝癸钠杂质B的合成方法

A New Method for Synthesizing Fondaparin Sodium Impurity B

磺达肝癸钠是一种Xa因子抑制剂,用于预防和治疗血栓类疾病。为了对磺达肝癸钠进行质量研究,我们采用化学合成的方法得到了磺达肝癸钠杂质B。该杂质是磺达肝癸钠的降解杂质,以往是从反应液粗品中分离纯化获取,但此杂质在粗品中的含量极低,很难大量得到。本合成方法采用简单易得的二糖为起始原料,经5步化学反应以较高的收率得到了杂质B,并通过NMR对其进行了表征。

Fondaparinux Sodium is a factor Xa inhibitor for the prevention and treatment of thrombotic diseases.In order to conduct a quality study on Fondaparinux Sodium,we made Fondaparin Sodium impurity B by chemical synthesis.Impurity B is a degradation impurity of Fondaparinux Sodium,which was normally obtained by separation and purification from the crude reaction medium.But the content of impurity B in the crude product is extremely low,and it is difficult to obtain it in large quantities.In our synthesis method with 5-step chemical reaction,a simple and easily available disaccharide is adopted as a starting material to produce impurity B in a high yield.