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HRID 1806211作成日:2026年10月26日

Ethyl Acetate → 3-[1-(ethylsulfonyl)-4-piperidinyl]-5-(4-formyl-2-thienyl)-1H-indole-7-carboxamide

https://huagongshe.com/reaction/1806211

反応式

関与物質

役割名称HCID仕込み量
反応物Ethyl AcetateHCID 8857—
反応物Potassium CarbonateHCID 11430—
反応物5-Bromothiophene-3-carbaldehydeHCID 12284894—
反応物3-[1-(ethylsulfonyl)-4-piperidinyl]-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole-7-carboxamideHCID 59828929—
触媒HCID 178418397HCID 178418397—
溶媒MethanolHCID 887—
溶媒WaterHCID 962—
溶媒1,4-DioxaneHCID 31275—
生成物3-[1-(ethylsulfonyl)-4-piperidinyl]-5-(4-formyl-2-thienyl)-1H-indole-7-carboxamideHCID 57732828161.8%

反応手順

To a solution of 5-bromo-3-thiophenecarbaldehyde (250 mg, 1.29 mmol) in dioxane (4.5 mL) and H2O (1.5 mL) was added 3-[1-(ethylsulfonyl)-4-piperidinyl]-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole-7-carboxamide (200 mg, 0.43 mmol), potassium carbonate (250 mg, 2.58 mmol) and tetrakis(triphenylphosphine)palladium (0) (56 mg, 0.049 mmol). The reaction was run in the microwave at 150° C. for 20 min. It was then treated with EtOAc and H2O to obtain the crude product. This was then treated with MeOH (10 mL) and the solid was filtered and collected to give 310 mg of the desired title compound.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08354406B2
出典データセットuspto-grants-2013_01
ORD IDord-c32ef290e0714211b7fd8600754abfb5
出典メモuspto-grants-2013_01