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HRID 559051作成日:2026年10月27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/559051

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 5747201387.4%

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 (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US08063058B2
出典データセットuspto-grants-2011_11
ORD IDord-8a22dc9e5a8043adb4aed2b37c4d2a6b
出典メモuspto-grants-2011_11