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HRID 1922161作成日:2026年10月27日

Dimethylformamide → (S)-2-[2-cyclopropyl-8-fluoro-4-methyl-3-(4-pyrazol-1-ylbenzyl)quinolin-5-yloxy]propionic acid methyl ester

https://huagongshe.com/reaction/1922161

反応式

関与物質

役割名称HCID仕込み量
反応物DimethylformamideHCID 6228—
反応物Potassium CarbonateHCID 11430—
反応物Methyl 2-chloropropanoate, (R)-HCID 149593—
反応物2-Cyclopropyl-8-fluoro-4-methyl-3-(4-pyrazol-1-ylbenzyl)quinolin-5-olHCID 136348363—
溶媒WaterHCID 962—
生成物(S)-2-[2-cyclopropyl-8-fluoro-4-methyl-3-(4-pyrazol-1-ylbenzyl)quinolin-5-yloxy]propionic acid methyl esterHCID 6745732141.9%

反応条件

温度40 °C

反応手順

A mixture of 2-cyclopropyl-8-fluoro-4-methyl-3-(4-pyrazol-1-ylbenzyl)quinolin-5-ol (0.064 g), N,N-dimethylformamide (0.86 mL), potassium carbonate (0.071 g) and (R)-2-chloropropionic acid methyl ester (0.032 g) was stirred at 40° C. for 3 days. The mixture was cooled to 0° C., diluted with water (40 mL) and extracted with ethyl acetate (3×10 mL). The combined extracts were washed saturated aqueous sodium chloride solution, dried over magnesium sulfate and concentrated under reduced pressure. Purification of the residue by column chromatography on silica gel, eluting with a mixture of ethyl acetate and cyclohexane (0:1 to 4:6 by volume) gave title compound as a colourless oil (0.033 g).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08173812B2
出典データセットuspto-grants-2012_05
ORD IDord-f84b059ec89642fcbc68e46ef12cdc15
出典メモuspto-grants-2012_05