Online article for Non-subscribers

Pay per view

Heterocycles has a pay-per-view service for Non-subscribers.
You will be able to directly purchase the full text article through PayPal.
Your purchased Paper can be downloaded after the payment is completed.
An e-mail will be sent the URL to download the paper.
If you have any questions, please contact:

Price: ¥ 4,400 (Yen only)
Period: This Article can be accessed for 7 days.

Short Paper | Regular issue | Vol 102, No. 9, 2021, pp.1797-1802
Published online, 2nd July, 2021
DOI: 10.3987/COM-21-14499
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


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.