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■ New and Practical Synthesis of GS-441524, the Key Intermediate of Remdesivir

Bo Li, Han Wang,* Cong Sun, Sheng Lu, LinLin Kang, and Shun Jiang

*College of Chemistry and Chemical Engineering, Shanghai University of Engineering Science, Shanghai 201620, China

Abstract

A new and practical synthesis of GS-441524, the key intermediate for remdesivir, is developed. 4-Amino-7-iodopyrrolo[2,1-f][1,2,4]triazine is protected by DMF-DMA, and reacted with 2,3,5-tri-O-benzyl-D-ribonolactone to give the product in 61% isolated yield. The next cyanation and debenzylation are carried out at −30 °C successively in 67% yield over two steps with >99% purity (HPLC). Purification methods of the intermediates and the final product involved in the route are developed.