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HRID 17470作成日:2026年10月26日

2-(Tributylstannyl)-1,3-thiazole → 7-Fluoro-5-methyl-6-phenyl-2-(1,3-thiazol-2-yl)-1,3-benzoxazole-4-carbonitrile

https://huagongshe.com/reaction/17470

反応式

関与物質

役割名称HCID仕込み量
反応物2-(Tributylstannyl)-1,3-thiazoleHCID 2763259—
反応物2-Chloro-7-fluoro-5-methyl-6-phenyl-1,3-benzoxazole-4-carbonitrileHCID 51041429—
反応物2,6-Di-t-butylcresolHCID 66637192—
触媒HCID 178418476HCID 178418476—
溶媒TolueneHCID 1140—
生成物7-Fluoro-5-methyl-6-phenyl-2-(1,3-thiazol-2-yl)-1,3-benzoxazole-4-carbonitrileHCID 6858442829.9%

反応条件

温度125 °C

反応手順

2-Tri-n-butylstannylthiazole (392 mg, 1.05 mmol), dichlorobis(triphenylphosphine)palladium(II) (49.0 mg, 0.070 mmol) and 2,6-di-tert-butylcresol (30.7 mg, 0.14 mmol) were added to a toluene (20 ml) solution of 2-chloro-7-fluoro-5-methyl-6-phenyl-1,3-benzoxazole-4-cabonitrile (I-130) (200 mg, 0.698 mmol), followed by heating under reflux in an oil bath at 125° C. for 5 hours in an argon atmosphere. The solvent was evaporated away under reduced pressure, then the residue was purified by silica gel column chromatography (eluent, hexane:ethyl acetate=9:1→2:1) to obtain the entitled compound (70.0 mg, 29.9%) as a pale yellow solid.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07737166B2
出典データセットuspto-grants-2010_06
ORD IDord-0047f5e8ceb241b98ab3b2476aa0cd4c
出典メモuspto-grants-2010_06