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A new scalable synthesis of entecavir
Tetrahedron ( IF 2.1 ) Pub Date : 2017-12-18 , DOI: 10.1016/j.tet.2017.12.034
Efthymia G. Gioti , Theocharis V. Koftis , Efstratios Neokosmidis , Elli Vastardi , Stefanos S. Kotoulas , Sakellarios Trakossas , Theodoros Tsatsas , Elizabeth E. Anagnostaki , Theodoros D. Panagiotidis , Constantinos Zacharis , Evanthia P. Tolika , Anastasia-Aikaterini Varvogli , Thanos Andreou , John K. Gallos

A new synthesis of entecavir from d-glucose in an average total yield of 3.5% was achieved via an intramolecular nitrile oxide cycloaddition (INOC) reaction and a Peterson olefination as key-steps. The present process was designed for industrial application, using widely available raw materials, simple and cheap reagents and avoiding low reaction temperatures, which are very common in the synthetic approaches towards similarly complex structures.



中文翻译:

恩替卡韦的新型可扩展合成

通过分子内腈氧化环加成(INOC)反应和彼得森烯化反应为关键步骤,由d-葡萄糖合成了恩替卡韦,平均总收率为3.5%。本方法是为工业应用而设计的,它使用了广泛可用的原料,简单且便宜的试剂并避免了低反应温度,这在合成类似结构的复杂方法中非常普遍。

更新日期:2017-12-18
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