由尿苷高产合成EIDD-2801。
A High-Yielding Synthesis of EIDD-2801 from Uridine.
作者信息
Steiner Alexander, Znidar Desiree, Ötvös Sándor B, Snead David R, Dallinger Doris, Kappe C Oliver
机构信息
Institute of Chemistry University of Graz, NAWI Graz Heinrichstrasse 28 8010 Graz Austria.
Center for Continuous Flow Synthesis and Processing (CCFLOW) Research Center Pharmaceutical Engineering GmbH (RCPE) Inffeldgasse 13 8010 Graz Austria.
出版信息
European J Org Chem. 2020 Nov 22;2020(43):6736-6739. doi: 10.1002/ejoc.202001340. Epub 2020 Nov 12.
A simple reordering of the reaction sequence allowed the improved synthesis of EIDD-2801, an antiviral drug with promising activity against the SARS-CoV-2 virus, starting from uridine. Compared to the original route, the yield was enhanced from 17 % to 61 %, and fewer isolation/purification steps were needed. In addition, a continuous flow procedure for the final acetonide deprotection was developed, which proved to be favorable toward selectivity and reproducibility.
对反应顺序进行简单重新排列后，从尿苷开始，可改进抗病毒药物EIDD - 2801（一种对SARS-CoV-2病毒具有潜在活性的药物）的合成。与原始路线相比，产率从17%提高到了61%，且所需的分离/纯化步骤更少。此外，还开发了用于最终缩酮脱保护的连续流动程序，该程序在选择性和重现性方面表现良好。
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