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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

反応式

関与物質

役割名称HCID仕込み量
反応物Potassium CarbonateHCID 11430—
反応物Isoquinoline-4-boronic acidHCID 3761204—
反応物N-(2-bromo-3,6-dimethylthieno[2,3-b]pyridin-4-yl)-3-chlorobenzenesulfonamideHCID 68324042—
触媒HCID 178418476HCID 178418476—
溶媒WaterHCID 962—
溶媒1,4-DioxaneHCID 31275—
生成物3-Chloro-N-[2-(4-isoquinolinyl)-3,6-dimethylthieno[2,3-b]pyridin-4-yl]benzenesulfonamideHCID 6832390737.2%

反応条件

温度100 °C

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

DOI10.6084/m9.figshare.5104873.v1
特許番号US09029545B2
出典データセットuspto-grants-2015_05
ORD IDord-df96f4948d40466e8266fbf0709b341c
出典メモuspto-grants-2015_05