Dey Supriya, Lo Hong-Jay, Wong Chi-Huey
Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, United States.
Org Lett. 2020 Jun 19;22(12):4638-4642. doi: 10.1021/acs.orglett.0c01386. Epub 2020 Jun 4.
The clinically approved Fondaparinux (Arixtra) has been used for the treatment of deep vein thrombosis and acute pulmonary embolism since 2002 and is considered to be better than the low-molecular weight heparin in terms of anticoagulation response, duration of action, and biosafety. However, the synthetic methods previously developed for its manufacture are relatively complicated, thus restricting its extensive use. We report here a potentially scalable and programmable one-pot synthesis of Fondaparinux using the [1,2,2] strategy and designed thioglycosides with well-defined reactivity as building blocks.
临床批准的磺达肝癸钠（安卓）自2002年起已用于治疗深静脉血栓形成和急性肺栓塞，并且在抗凝反应、作用持续时间和生物安全性方面被认为优于低分子量肝素。然而，先前开发的用于其制造的合成方法相对复杂，因此限制了其广泛使用。我们在此报告一种使用[1,2,2]策略和设计的具有明确反应性的硫代糖苷作为构建块的潜在可扩展且可编程的一锅法合成磺达肝癸钠。
