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HRID 1499435作成日:2026年10月25日

Hydrochloric Acid → 3-Amino-6-(2,6-difluorophenyl)-5-fluoropicolinic acid

https://huagongshe.com/reaction/1499435

反応式

関与物質

役割名称HCID仕込み量
反応物Hydrochloric AcidHCID 313—
反応物TetrahydrofuranHCID 8028—
反応物Lithium hydroxide, monohydrateHCID 168937—
反応物Methyl 3-amino-6-(2,6-difluorophenyl)-5-fluoropicolinateHCID 59226608—
溶媒WaterHCID 962—
生成物3-Amino-6-(2,6-difluorophenyl)-5-fluoropicolinic acidHCID 5922651386%

反応条件

温度50 °C

反応手順

To a mixture of methyl 3-amino-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxylate (84.0 mg, 0.298 mmol) and lithium hydroxide, monohydrate (40.2 mg, 0.958 mmol), THF (2.0 mL) was added followed by water (1.0 mL). The mixture was heated at 50° C. for 3 h. The reaction was then cooled to 0° C. for, and 1 M HCl was added slowly until the pH reached 2. The reaction mixture was then diluted with water (20 mL), extracted with EtOAc (3×20 mL), and the combined organic extract was washed with brine (30 mL), dried over Na2SO4, and concentrated under reduced pressure to give the sub-title compound as a white solid (68.5 mg, 86%). LCMS calc. for C12H8F3N2O2 (M+H)+: m/z=269.0. found 269.0.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US09200004B2
出典データセットuspto-grants-2015_12
ORD IDord-72612c69293f44c0a25b7c8d56717e01
出典メモuspto-grants-2015_12