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Potassium Carbonate → 6-bromo-1-[1-(2,6-dichloro-3-fluorophenyl)ethoxy]-1H-pyrrolo[3,2-b]pyridine
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Potassium Carbonate | HCID 11430 | — |
| 反応物 | Diethyl 2-(5-bromo-3-nitropyridin-2-yl)malonate | HCID 57516275 | — |
| 反応物 | 1-(2,6-Dichloro-3-fluorophenyl)ethyl methanesulfonate | HCID 58532496 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | 6-bromo-1-[1-(2,6-dichloro-3-fluorophenyl)ethoxy]-1H-pyrrolo[3,2-b]pyridine | HCID 67458418 | 78% |
反応手順
A solution of 1-(2,6-dichloro-3-fluorophenyl)ethyl methanesulfonate (4.39 g, 15.3 mmol, 1.0 eq), 6-bromo-1H-pyrrolo[3,2-b]pyridin-1-ol (prepared as in example 1: 3.92 g, 20.0 mmol, 1.3 eq) and K2CO3 (6.34 g, 45.9 mmol, 3.0 eq) in 90 ml of N,N-dimethylformamide (DMF) was stirred at room temperature overnight. The solid was filtered out and the solvent evaporated. The residue was dissolved in DCM, and the solution was washed with water and brine, dried, evaporated and chromatographed (MeOH/DCM 1:20) to give a light yellow oil, 4.63 g, in 78% yield.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08912330B2 |
| 出典データセット | uspto-grants-2014_12 |
| ORD ID | ord-b14a655b409c405baae399dddaf72956 |
| 出典メモ | uspto-grants-2014_12 |