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HRID 516439作成日:2026年10月24日

Methanol → 5-(4-Methoxybenzyloxy)-1-methyl-1H-pyrazole-3-carboxylic Acid

https://huagongshe.com/ja/reaction/516439

反応式

関与物質

役割名称HCID仕込み量
反応物MethanolHCID 887—
反応物WaterHCID 962—
反応物Lithium HydroxideHCID 3939—
反応物DimethylformamideHCID 6228—
反応物Potassium CarbonateHCID 11430—
反応物4-Methyloxybenzyl chlorideHCID 69993—
反応物HCID 178498595HCID 178498595—
生成物5-(4-Methoxybenzyloxy)-1-methyl-1H-pyrazole-3-carboxylic AcidHCID 86705138133.5%

反応条件

温度60 °C

反応手順

To a stirred solution of 5-hydroxy-1-methyl-1H-pyrazole-3-carboxylic acid methyl ester (200 mg, 1 mmol) in DMF (992 μL, 12.8 mmol) at 0° C. was added K2CO3 (195 mg, 1.4 mmol). After 10 minutes at 0° C. p-methoxybenzyl chloride (208 μL, 1.5 mmol) was added, and the resulting mixture was stirred at 60° C. for 1 hour, before allowing to cool to room temperature. MeOH (2.6 mL, 63.2 mmol) was added, followed by LiOH (61.4 mg, 2.6 mmol) in water (2.6 mL, 142 mmol), and the reaction was monitored for completion. The solvent was removed in vacuo. Water was added to the vial and the crude product was acidified with a 1N HCl aqueous solution. The solids were filtered to yield the title compound as a white solid (350 mg).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US09108934B2
出典データセットuspto-grants-2015_08
ORD IDord-cf357ab4236c474faedb844cdd8ff300
出典メモuspto-grants-2015_08