Programmable One-Pot Synthesis of Heparin Pentasaccharide Fondaparinux
Programmable One-Pot Synthesis of Heparin Pentasaccharide Fondaparinux
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DOI：
10.1021/acs.orglett.0c01386
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发表时间：
2020-06-19
期刊：
影响因子：
5.2
通讯作者：
Wong, Chi-Huey
中科院分区：
文献类型：
--
作者：
Dey, Supriya;Lo, Hong-Jay;Wong, Chi-Huey
临床批准的Fondaparinux （Arixtra）自2002年以来一直用于治疗深静脉血栓和急性肺栓塞，在抗凝反应、作用时间和生物安全性方面被认为优于低分子量肝素。然而，以往为其制造而开发的合成方法相对复杂，限制了其广泛使用。我们在这里报告了一种潜在的可扩展和可编程的一锅合成Fondaparinux的方法，使用[1,2,2]策略，并设计了具有明确反应性的巯基糖苷作为构建块。
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.