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HRID 2201034作成日:2026年10月24日

Hydrogen Peroxide → 4-((1R,2S)-2-aminocyclohexylamino)-2-(1-methyl-1H-pyrazol-4-ylamino)benzamide

https://huagongshe.com/ja/reaction/2201034

反応式

関与物質

役割名称HCID仕込み量
反応物Hydrogen PeroxideHCID 784—
反応物WaterHCID 962—
反応物Potassium CarbonateHCID 11430—
反応物tert-butyl (1S,2R)-2-(4-cyano-3-(1-methyl-1H-pyrazol-4-ylamino)phenylamino)cyclohexylcarbamateHCID 68077202—
溶媒Dimethyl SulfoxideHCID 679—
溶媒Ethyl AcetateHCID 8857—
生成物4-((1R,2S)-2-aminocyclohexylamino)-2-(1-methyl-1H-pyrazol-4-ylamino)benzamideHCID 5733433578.7%

反応手順

To a solution of tert-butyl (1S,2R)-2-(4-cyano-3-(1-methyl-1H-pyrazol-4-ylamino)phenylamino)cyclohexylcarbamate (50 mg, 0.12 mmol) in DMSO (1 mL), K2CO3 (100 mg, 0.724 mmol) and H2O2 (50% aq., 0.800 mL) were added. The mixture was stirred at 100 C for 10 min. Water and EtOAc were added. The organic phase was separated, dried over Na2SO4, concentrated in vacuo. The residue was dissolved in TFA (1 mL). After 10 min of standing, TFA was removed in vacuo. The residue was purified by HPLC to give the titled compound (31 mg). MS 329.4 (M+H); UV 205.3, 258.4, 280.5, 327.9 nm

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US09359375B2
出典データセットuspto-grants-2016_06
ORD IDord-5ee65d6d35a948b2a7ca22b8eef6caca
出典メモuspto-grants-2016_06