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HRID 81359作成日:2026年10月26日

2-Fluorophenol → 5-(2-Fluoro-phenoxy)-2-(4-methoxy-3,5-dimethyl-phenyl)-oxazolo[5,4-d]pyrimidine

https://huagongshe.com/reaction/81359

反応式

関与物質

役割名称HCID仕込み量
反応物2-FluorophenolHCID 9707—
反応物Sodium hydrideHCID 24758—
反応物5-Chloro-2-(4-methoxy-3,5-dimethylphenyl)oxazolo[5,4-d]pyrimidineHCID 86675954—
溶媒DimethylacetamideHCID 31374—
生成物5-(2-Fluoro-phenoxy)-2-(4-methoxy-3,5-dimethyl-phenyl)-oxazolo[5,4-d]pyrimidineHCID 53311373—

反応手順

149 mg of sodium hydride were added under an argon atmosphere to a solution of 418 mg of 2-fluoro-phenol in 15 ml dimethylacetamide. After stirring for 30 min at room temperature a solution of 900 mg of 5-chloro-2-(4-methoxy-3,5-dimethyl-phenyl)-oxazolo[5,4-d]pyrimidine in 20 ml dimethylacetamide was added slowly. The mixture was allowed to stir for 1.5 h at room temperature. Upon consumption of the starting oxazolo[5,4-d]pyrimidine an aqueous solution of citric acid (100 g/l) was added until the pH was neutral. The aqueous layer was extracted twice with 15 ml of ethyl acetate. The combined organic layers were dried over sodium sulfate, filtered and the solvents were removed in vacuo. The title compound was isolated by silica gel chromatography (heptane/ethyl acetate gradient) as a white solid. Yield: 820 mg.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08846690B2
出典データセットuspto-grants-2014_09
ORD IDord-b0a87601989c458e9eb5b0a7ac85ad9f
出典メモuspto-grants-2014_09