A Scalable Synthesis of Roxadustat (FG-4592),Organic Process Research & Development

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A Scalable Synthesis of Roxadustat (FG-4592)
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2021-08-17 , DOI: 10.1021/acs.oprd.1c00281
Ondřej Píša ₁ , Stanislav Rádl ₁ , Igor Čerňa ₁ , Filip Šembera ₁

Affiliation

A scalable five-step protocol for synthesis of roxadustat, an orally administered hypoxia-inducible factor-propyl hydroxylase inhibitor (HIF-PHI), was developed with an emphasis placed on aspects of medicinal chemistry. The isoquinoline core of the molecule was prepared using a purposefully designed cyclocondensation in which both the cyclocondensation and demasking of the groups being condensed is promoted by a common acid agent in one step. Roxadustat was obtained pure in a very competitive overall yield across all reaction steps and in compliance with permissible residual Pd level in API.

中文翻译：

Roxadustat (FG-4592) 的可扩展合成

开发了一种可扩展的五步法合成罗沙司他，一种口服的缺氧诱导因子-丙基羟化酶抑制剂 (HIF-PHI)，重点放在药物化学的各个方面。该分子的异喹啉核心是使用有目的设计的环缩合制备的，其中缩合基团的环缩合和去掩蔽均由一种常见的酸剂在一个步骤中促进。Roxadustat 在所有反应步骤中以极具竞争力的总收率获得纯品，并符合 API 中允许的残留 Pd 水平。

更新日期：2021-08-17

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