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HRID 84794作成日:2026年10月26日

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

https://huagongshe.com/reaction/84794

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-indol-4-ylamino)phenylamino)cyclohexylcarbamateHCID 69283979—
溶媒Dimethyl SulfoxideHCID 679—
溶媒Ethyl AcetateHCID 8857—
生成物4-((1R,2S)-2-aminocyclohexylamino)-2-(1-methyl-1H-indol-4-ylamino)benzamideHCID 5733402613.9%

反応手順

To a solution of tert-butyl (1S,2R)-2-(4-cyano-3-(1-methyl-1H-indol-4-ylamino)phenylamino)cyclohexylcarbamate (90 mg, 0.19 mmol) in DMSO (2 mL). K2CO3 (130 mg, 0.94 mmol) and H2O2 (50% aq., 0.500 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 (2 mL). After 10 min of standing, TFA was removed in vacuo. The residue was purified by HPLC to give the titled compound (10 mg). MS 378.3 (M+H); UV 224.7, 291.5 nm

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08846928B2
出典データセットuspto-grants-2014_09
ORD IDord-cb73c02deddc499bb962f4b456490400
出典メモuspto-grants-2014_09