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HRID 84917作成日:2026年10月26日

Acetic Acid → (R)-4-(1-amino-3-cyclopropyl-1-oxopropan-2-ylamino)-5-fluoro-2-(3-phenylisoxazol-5-ylamino)benzamide

https://huagongshe.com/reaction/84917

反応式

関与物質

役割名称HCID仕込み量
反応物Acetic AcidHCID 176—
反応物Hydrogen PeroxideHCID 784—
反応物Sodium HydroxideHCID 14798—
反応物(R)-2-(4-cyano-2-fluoro-5-(3-phenylisoxazol-5-ylamino)phenylamino)-3-cyclopropylpropanamideHCID 67508272—
溶媒Dimethyl SulfoxideHCID 679—
溶媒EthanolHCID 702—
生成物(R)-4-(1-amino-3-cyclopropyl-1-oxopropan-2-ylamino)-5-fluoro-2-(3-phenylisoxazol-5-ylamino)benzamideHCID 67516525—

反応手順

To a solution of (R)-2-(4-cyano-2-fluoro-5-(3-phenylisoxazol-5-ylamino)phenylamino)-3-cyclopropylpropanamide (75 mg) in EtOH (1 mL) and DMSO (0.5 mL) at room temperature, aq. 1N NaOH (0.5 mL) and aq. H2O2 (50%, 0.5 mL) were added. The mixture was stirred at room temperature for 15 min. HOAc (0.5 mL) was added. After being concentrated in vacuo, the residue was purified by HPLC to give the titled compound (13 mg). MS 424.4 (M+H); UV 201.0, 244.9, 289.1 nm; t 0.668 min.

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-357775f09b9a43e888d3ed59288a0a6e
出典メモuspto-grants-2014_09