Development of a Robust and Scalable Process for the Large-Scale Preparation of Vadadustat,Organic Process Research & Development

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Development of a Robust and Scalable Process for the Large-Scale Preparation of Vadadustat
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2021-03-05 , DOI: 10.1021/acs.oprd.1c00004
Biyue Lin ₁ , Jingping Kou ₁ , Shuming Wu _{1,

2} , Xuerong Cai ₁ , Qingbo Xiao ₁ , Yinglong Li ₁ , Jian Hu ₁ , Jianbing Li ₁ , Zhongqing Wang _{1,

2,

3}

Affiliation

A novel and scalable process is developed for the industrial synthesis of vadadustat. The four-step process is one step shorter compared to the reported routes with an increase in total yield to 49.1%. Detailed optimizations furnish vadadustat with a purity of >99.5% through cross-coupling, aromatic substitution and nitrile hydrolysis, amidation, and ester-ether deprotection. The process is also robust and was demonstrated in a kilogram laboratory. Meanwhile, the corresponding impurity profile was thus studied in detail and well documented.

中文翻译：

开发鲁棒且可扩展的Vadadustat大规模制备方法

开发了一种新颖且可扩展的方法，用于工业化vadadustat。与报告的路线相比，四步过程缩短了一步，总收率提高到49.1％。通过交叉偶联，芳族取代和腈水解，酰胺化和酯醚脱保护作用，详细的优化工艺可提供纯度> 99.5％的Vadadustat。该过程也很可靠，并在公斤实验室中得到了证明。同时，对相应的杂质分布进行了详细研究并充分记录在案。

更新日期：2021-04-16

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