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HRID 384256作成日:2026年10月26日

1,2-Dichloroethane → 2-(1H-benzo[d][1,2,3]triazol-1-yloxy)-4-(1-methyl-1H-indol-4-ylamino)pyrimidine-5-carboxamide

https://huagongshe.com/reaction/384256

反応式

関与物質

役割名称HCID仕込み量
反応物1,2-DichloroethaneHCID 11—
反応物AmmoniaHCID 222—
反応物1-HydroxybenzotriazoleHCID 75771—
反応物2-chloro-4-(1-methyl-1H-indol-4-ylamino)pyrimidine-5-carboxylic acidHCID 57472012—
溶媒WaterHCID 962—
溶媒DimethylformamideHCID 6228—
溶媒Ethyl AcetateHCID 8857—
生成物2-(1H-benzo[d][1,2,3]triazol-1-yloxy)-4-(1-methyl-1H-indol-4-ylamino)pyrimidine-5-carboxamideHCID 57472013—

反応手順

To a solution of 2-chloro-4-(1-methyl-1H-indol-4-ylamino)pyrimidine-5-carboxylic acid (325 mg, 1.08 mmol) and HOBt.H2O (198 mg, 1.29 mmol) in DMF (4 mL), EDC (248 mg, 1.29 mmol) was added. The mixture was stirred at room temperature for 1.5 h. Ammonia (0.5 M in dioxane, 8.00 mL, and 4.00 mmol) was added. It was stirred at room temperature overnight. Water and EtOAc were added. The organic phase was separated, washed with 1 N HCl, then with 5% NaHCO3, dried over Na2SO4, concentrated in vacuo to give 2-(1H-benzo[d][1,2,3]triazol-1-yloxy)-4-(1-methyl-1H-indol-4-ylamino)pyrimidine-5-carboxamide (378 mg). MS 401.4 (M+H)

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08367689B2
出典データセットuspto-grants-2013_02
ORD IDord-95c722ed837f4a5ebdd20194cb5a5d03
出典メモuspto-grants-2013_02