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HRID 655338作成日:2026年10月25日

Triphenylphosphine → 5-methyl-3-{3-[5-(4-methylpiperazin-1-yl)pyrimidin-2-yl]benzyl}-3H-oxazolo[4,5-b]pyridin-2-one

https://huagongshe.com/reaction/655338

反応式

関与物質

役割名称HCID仕込み量
反応物TriphenylphosphineHCID 11776—
反応物Di-tert-butyl azodicarboxylateHCID 97268—
反応物5-Methyloxazolo[4,5-b]pyridin-2(3H)-oneHCID 10012075—
反応物{3-[5-(4-Methylpiperazin-1-yl)pyrimidin-2-yl]phenyl}methanolHCID 59484860—
溶媒DimethylformamideHCID 6228—
生成物5-methyl-3-{3-[5-(4-methylpiperazin-1-yl)pyrimidin-2-yl]benzyl}-3H-oxazolo[4,5-b]pyridin-2-oneHCID 58486104—

反応手順

67 mg (0.44 mmol) of 5-methyl-3H-oxazolo[4,5-b]pyridin-2-one and 125 mg (0.44 mmol) of {3-[5-(4-methylpiperazin-1-yl)pyrimidin-2-yl]phenyl}methanol are suspended in 5 ml of DMF with 222 mg (0.67 mmol) of polymer-bound triphenylphosphine (about 3 mmol of triphenylphosphine per g), and the mixture is shaken at room temperature for 30 min. 156 mg (0.67 mmol) of di-tert-butyl azodicarboxylate are added. The reaction mixture is shaken at room temperature for 15 h. The reaction mixture is filtered, the residue is evaporated, and the residue is purified by column chromatography on silica gel, giving 67 mg of “A125”; HPLC: Rt=2.26 min (method B); ESI: 418 (M+H);

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08071593B2
出典データセットuspto-grants-2011_12
ORD IDord-51384a395767447e990e66c19e294b6d
出典メモuspto-grants-2011_12