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用于无钯合成抗疟药 MMV048 的戊脒盐化学应用:一种“自下而上”的方法。

Application of Vinamidinium Salt Chemistry for a Palladium Free Synthesis of Anti-Malarial MMV048: A "Bottom-Up" Approach.

机构信息

Medicines for All Institute, 737 North Fifth Street, Box 980100, Richmond, Virginia 23298, United States.

WuXi AppTec (Wuhan) Co. Ltd., Wuhan East Lake High-tech Development Zone, Wuhan 430075, P. R. of China.

出版信息

Org Lett. 2021 Jul 16;23(14):5400-5404. doi: 10.1021/acs.orglett.1c01725. Epub 2021 Jun 29.

Abstract

MMV390048 () is a clinical compound under investigation for antimalarial activity. A new synthetic route was developed which couples two aromatic fragments while forming the central pyridine ring over two steps. This sequence takes advantage of raw materials used in the existing etoricoxib supply chain and eliminates the need for palladium catalysts, which were projected to be major cost-drivers.

摘要

MMV390048()是一种正在研究用于抗疟活性的临床化合物。开发了一种新的合成途径,该途径通过两步反应将两个芳族片段偶联,同时形成中心吡啶环。该序列利用了现有依托考昔供应链中使用的原料,并消除了对钯催化剂的需求,钯催化剂预计将成为主要的成本驱动因素。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/12dd/9385109/d1f4e9f78f2d/ol1c01725_0005.jpg

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