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HRID 518406作成日:2026年10月26日

Water → 3-(Cyclopropylmethoxy)-2-iodo-6-methylsulfonylpyridine

https://huagongshe.com/reaction/518406

反応式

関与物質

役割名称HCID仕込み量
反応物WaterHCID 962—
反応物Potassium CarbonateHCID 11430—
反応物BromomethylcyclopropaneHCID 81503—
反応物2-Iodo-6-methylsulfonylpyridin-3-olHCID 118022372—
溶媒AcetonitrileHCID 6342—
生成物3-(Cyclopropylmethoxy)-2-iodo-6-methylsulfonylpyridineHCID 11802251684.8%

反応条件

温度80 °C

反応手順

A mixture of 2-iodo-6-methylsulfonylpyridin-3-ol (500.0 mg, 1.67 mmol), bromomethylcyclopropane (248.4 mg, 1.84 mmol) and K2CO3 (461.3 mg, 33.4 mmol) in ACN (15 mL) was stirred at 80° C. for 4 hrs. Water (30 mL) was added and the mixture was extracted with EtOAc (30 mL×3). The combined organic layers were washed with brine (30 mL), dried over Na2SO4, filtered and concentrated to give the title compound (500.0 mg, 84.8%). 1H NMR (CDCl3, 400 MHz) δ 7.96 (d, J=8.8 Hz, 1H), 7.52 (d, J=8.4 Hz, 1H), 4.09 (d, J=6.8 Hz, 2H), 3.22 (s, 3H), 1.36-1.22 (m, 1H), 0.69-0.57 (m, 2H), 0.43-0.37 (m, 2H). LCMS: 354.0 (M+1)+

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US09115114B2
出典データセットuspto-grants-2015_08
ORD IDord-cbaca222dea84f609941eca25eeba7e9
出典メモuspto-grants-2015_08