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A new scalable synthesis of entecavir

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Abstract 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… Click to show full abstract

Abstract 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.

Keywords: synthesis entecavir; new scalable; scalable synthesis; synthesis

Journal Title: Tetrahedron
Year Published: 2018

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