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HRID 1806258作成日:2026年10月25日

Potassium Carbonate → 5-(3-cyano-5-formylphenyl)-3-[1-(ethylsulfonyl)-4-piperidinyl]-1H-indole-7-carboxamide

https://huagongshe.com/reaction/1806258

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3-Bromo-5-formylbenzonitrileHCID 53425523—
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PalladiumHCID 23938—
触媒HCID 178418397HCID 178418397—
溶媒1,4-DioxaneHCID 31275—
生成物5-(3-cyano-5-formylphenyl)-3-[1-(ethylsulfonyl)-4-piperidinyl]-1H-indole-7-carboxamideHCID 86631024—

反応条件

温度160 °C

反応手順

To a solution of 3-[1-(ethylsulfonyl)-4-piperidinyl]-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole-7-carboxamide (46 mg, 0.1 mmol) in dioxane (2.0 mL, 0.7 mL) was added 3-bromo-5-formylbenzonitrile (68 mg, 0.3 mmol) and K2CO3 (83 mg, 0.6 mmol) in a microwave tube. The reaction mixture was degassed for 5 min before addition of tetrakis (triphenylphosphosphine) palladium (0) (11 mg, 0.01 mmol). The reaction was heated in a microwave for 20 min at 160° C. It was then purified by Gilson Preparatory HPLC to give 5-(3-cyano-5-formylphenyl)-3-[1-(ethylsulfonyl)-4-piperidinyl]-1H-indole-7-carboxamide.

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-a94b003ebe9744768d29d3f3654063b8
出典メモuspto-grants-2013_01