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HRID 531760作成日:2026年10月27日

Chloroacetamide → 2-(4-(5-(3-(1-(3,5-difluorobenzyl)-1H-pyrazol-4-yl)-1-tosyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyridin-2-yl)piperazin-1-yl) acetamide

https://huagongshe.com/reaction/531760

反応式

関与物質

役割名称HCID仕込み量
反応物ChloroacetamideHCID 6580—
反応物Sodium BicarbonateHCID 516892—
反応物3-(1-(3,5-difluorobenzyl)-1H-pyrazol-4-yl)-5-(6-(piperazin-1-yl)pyridin-3-yl)-1-tosyl-1H-pyrrolo[2,3-b]pyridineHCID 90031541—
反応物3-(1-(3,5-difluorobenzyl)-1H-pyrazol-4-yl)-5-(6-(4-methylpiperazin-1-yl)pyridin-3-yl)-1H-pyrrolo[2,3-b]pyridineHCID 90064901—
溶媒Acetone ethanolHCID 21889777—
生成物2-(4-(5-(3-(1-(3,5-difluorobenzyl)-1H-pyrazol-4-yl)-1-tosyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyridin-2-yl)piperazin-1-yl) acetamideHCID 9003149791.7%

反応手順

Using similar reaction conditions as described in step-i of example-82A, 3-(1-(3,5-difluorobenzyl)-1H-pyrazol-4-yl)-5-(6-(piperazin-1-yl)pyridin-3-yl)-1-tosyl-1H-pyrrolo[2,3-b]pyridine (step 2 compound of example 133) (100 mg, 0.16 mmol) was alkylated using 2-chloroacetamide (30 mg, 0.32 mmol), sodium bicarbonate (40 mg, 0.48 mmol) and ethanol/acetone (3/3 mL) to get 100 mg (91.7%) of the titled compound after purification by column (Silica gel 60/120) using 5% methanol in dichloromethane as eluent. MS: m/z=683.3 (M+1).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US09353107B2
出典データセットuspto-grants-2016_05
ORD IDord-95063ae21a7f4516a0d498acbf8a64b8
出典メモuspto-grants-2016_05