Paymode Dinesh J, Cardoso Flavio S P, Agrawal Toolika, Tomlin John W, Cook Daniel W, Burns Justina M, Stringham Rodger W, Sieber Joshua D, Gupton B Frank, Snead David R
Chemical Development, Medicines for All Institute, 737 North Fifth Street, Box 980100, Richmond, Virginia 23298-0100, United States.
Analytical Development, Medicines for All Institute, 737 North Fifth Street, Box 980100, Richmond, Virginia 23298-0100, United States.
Org Lett. 2020 Oct 2;22(19):7656-7661. doi: 10.1021/acs.orglett.0c02848. Epub 2020 Sep 15.
Pyrrolotriazine is an important precursor to remdesivir. Initial results toward an efficient synthesis are disclosed consisting of sequential cyanation, amination, and triazine formation beginning from pyrrole. This route makes use of highly abundant, commoditized raw material inputs. The yield of triazine was doubled from 31% to 59%, and the synthetic step count was reduced from 4 to 2. These efforts help to secure the remdesivir supply chain.
吡咯并三嗪是瑞德西韦的重要前体。本文披露了一种高效合成方法的初步结果,该方法从吡咯开始,依次进行氰化、胺化和三嗪形成反应。此路线使用了大量丰富的商品化原料。三嗪的产率从31%提高到了59%,合成步骤从4步减少到了2步。这些努力有助于确保瑞德西韦的供应链。