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HRID 573655作成日:2026年10月26日
Potassium Carbonate → 3-Chloro-N-[2-(4-isoquinolinyl)-3,6-dimethylthieno[2,3-b]pyridin-4-yl]benzenesulfonamide
https://huagongshe.com/reaction/573655
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Potassium Carbonate | HCID 11430 | — |
| 反応物 | Isoquinoline-4-boronic acid | HCID 3761204 | — |
| 反応物 | N-(2-bromo-3,6-dimethylthieno[2,3-b]pyridin-4-yl)-3-chlorobenzenesulfonamide | HCID 68324042 | — |
| 触媒 | HCID 178418476 | HCID 178418476 | — |
| 溶媒 | Water | HCID 962 | — |
| 溶媒 | 1,4-Dioxane | HCID 31275 | — |
| 生成物 | 3-Chloro-N-[2-(4-isoquinolinyl)-3,6-dimethylthieno[2,3-b]pyridin-4-yl]benzenesulfonamide | HCID 68323907 | 37.2% |
反応手順
To a solution of N-(2-bromo-3,6-dimethylthieno[2,3-b]pyridin-4-yl)-3-chlorobenzenesulfonamide (Example 77) (100 mg, 0.232 mmol) in 1,4-dioxane (2 mL) and water (1 mL) was added 4-isoquinolinylboronic acid (40.1 mg, 0.232 mmol), bis(triphenylphosphine)palladium(II) chloride (16.26 mg, 0.023 mmol) and potassium carbonate (112 mg, 0.811 mmol) and the mixture heated at 100° C. for 1 h using a microwave reactor. The mixture was then filtered through celite, washing with ethyl acetate (30 mL) and the filtrate evaporated to dryness. The residue was then purified by MDAP (acidic conditions), to afford the title compound (41.45 mg). LCMS (A) m/z: 480 [M+1]+, Rt 1.13 min (acidic).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US09029545B2 |
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| 出典データセット | uspto-grants-2015_05 |
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| ORD ID | ord-df96f4948d40466e8266fbf0709b341c |
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| 出典メモ | uspto-grants-2015_05 |
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