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3-fluoro-5-methoxypicolinic acid synthesis

3synthesis methods
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Yield:1227511-52-5 57%

Reaction Conditions:

Stage #1: 3-fluoro-5-methoxypicolinic acid methyl esterwith water;lithium hydroxide in tetrahydrofuran at 25; for 0.5 h;
Stage #2: with citric acid in tetrahydrofuran;water; pH=5;

Steps:

A4.3

To A4-2 (0.059 g, 0.32 mmol) in THF was added 2N LiOH (0.5 mL, 1 mmol).The reaction was stirred at room temperature for 30 minutes. The reaction was adjusted to pH~5 with saturated citric acid(aq). Brine was added and the mixture was extracted with EtO Ac. The combined organic layers were washed with brine, dried (MgS04), filtered, and concentrated in vacuo to provide A4-4 (0.031 g, 57%).

References:

WO2012/138734,2012,A1 Location in patent:Page/Page column 66