Three-Step Continuous\nFlow Synthesis of the Intermediate\n4‑Fluoro-2-methoxy-5-nitrophenol of Linzagolix

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

Publication Details

Journal
Figshare
Published
2024-12-18
DOI
https://doi.org/10.1021/acs.oprd.4c00405.s001
Primary Topic
Pasture and Agricultural Systems
Type
article
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0.00
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article

Three-Step Continuous\nFlow Synthesis of the Intermediate\n4‑Fluoro-2-methoxy-5-nitrophenol of Linzagolix

Figshare
Pasture and Agricultural Systems
article

Three-Step Continuous\nFlow Synthesis of the Intermediate\n4‑Fluoro-2-methoxy-5-nitrophenol of Linzagolix

article en

Abstract

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

Figshare
Clean water and sanitation
Openalex Percentile: Top 37%
Pasture and Agricultural Systems
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Three-Step Continuous\nFlow Synthesis of the Intermediate\n4‑Fluoro-2-methoxy-5-nitrophenol of Linzagolix · Figshare (2024) | TGRS Research Map | TGRS