应用Vinamidinium盐化学无钯合成抗疟疾药物MMV048:“自下而上”的方法

IF 4.9 1区化学 Q1 CHEMISTRY, ORGANIC Organic Letters Pub Date : 2021-06-29 DOI:10.1021/acs.orglett.1c01725

Dinesh J. Paymode, Le Chang, Dan Chen, Binglin Wang, Komirishetty Kashinath, Vijayagopal Gopalsamuthiram, D. Tyler McQuade, N. Vasudevan, Saeed Ahmad, David R. Snead*

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引用次数: 3

摘要

MMV390048(1)是一种临床研究中的抗疟疾活性化合物。提出了一种新的合成路线，将两个芳香片段偶联，分两步形成中心吡啶环。该流程利用了现有etoricoxib供应链中使用的原材料，并消除了钯催化剂的需求，钯催化剂被认为是主要的成本驱动因素。

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

MMV390048 (1) 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.

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来源期刊

Organic Letters 化学-有机化学

CiteScore

9.30

自引率

11.50%

发文量

1607

审稿时长

1.5 months

期刊介绍： Organic Letters invites original reports of fundamental research in all branches of the theory and practice of organic, physical organic, organometallic,medicinal, and bioorganic chemistry. Organic Letters provides rapid disclosure of the key elements of significant studies that are of interest to a large portion of the organic community. In selecting manuscripts for publication, the Editors place emphasis on the originality, quality and wide interest of the work. Authors should provide enough background information to place the new disclosure in context and to justify the rapid publication format. Back-to-back Letters will be considered. Full details should be reserved for an Article, which should appear in due course.