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HRID 72448作成日:2026年10月26日

Acetonitrile → Methyl 2-(3-((5-methylisoxazol-3-yl)oxy)azetidin-1-yl)-5-(trifluoromethyl)nicotinate

https://huagongshe.com/reaction/72448

反応式

関与物質

役割名称HCID仕込み量
反応物AcetonitrileHCID 6342—
反応物HymexazolHCID 24781—
反応物Methyl 2-(3-((methylsulfonyl)oxy)azetidin-1-yl)-5-(trifluoromethyl)nicotinateHCID 86697871—
生成物Methyl 2-(3-((5-methylisoxazol-3-yl)oxy)azetidin-1-yl)-5-(trifluoromethyl)nicotinateHCID 6795846616.5%

反応条件

温度180 °C

反応手順

To a solution of 5-methylisoxazol-3-ol (33.48 mg, 0.34 mmol) in acetonitrile (0.7 ml) potassium carbonate (60.85 mg, 0.44 mmol) was added followed by addition of methyl 2-(3-((methylsulfonyl)oxy)azetidin-1-yl)-5-(trifluoromethyl)nicotinate (D68) (120 mg, 0.34 mmol). The reaction mixture was heated at 180° C. under microwave irradiation for 25 min. After solvent evaporation the residue was purified by Biotage SNAP-Si column (10 g) eluting with cycloexane/ethyl acetate from 95/05 to 70/30. Collected fractions were evaporated in vacuo tot afford the title compound (D88) (20 mg)

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08828987B2
出典データセットuspto-grants-2014_09
ORD IDord-b976eb125a6d42849a39235dbb30c1df
出典メモuspto-grants-2014_09