4-Fluoro-2-methoxy-5-nitrophenol is a key intermediate of the GnRH receptor antagonist Linzagolix. The traditional synthetic methods have several disadvantages including prolonged reaction time and safety issues. Herein, we describe a three-step continuous flow synthesis of 4-fluoro-2-methoxy-5-nitrophenol via esterification, nitration, and hydrolysis. The total residence time was 234 s, and the total yield was 85.6%, which substantially reduced the reaction time and considerably improved the process safety as well as the total yield.

中文翻译：

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Linzagolix 中间体 4-氟-2-甲氧基-5-硝基苯酚的三步连续流合成


4-氟-2-甲氧基-5-硝基苯酚是 GnRH 受体拮抗剂 Linzagolix 的关键中间体。传统的合成方法有几个缺点，包括反应时间长和安全问题。在本文中，我们描述了通过酯化、硝化和水解实现 4-氟-2-甲氧基-5-硝基苯酚的三步连续流合成。总停留时间为 234 s，总产率为 85.6%，这大大缩短了反应时间，并显著提高了工艺安全性和总产率。