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HRID 58231作成日:2026年10月25日

Sodium Carbonate → HCID 178456859、化合物

https://huagongshe.com/reaction/58231

反応式

関与物質

役割名称HCID仕込み量
反応物Sodium CarbonateHCID 10340—
反応物(5-Fluoropyridin-3-yl)boronic acidHCID 44717403—
反応物HCID 178456860HCID 178456860—
触媒HCID 178418397HCID 178418397—
溶媒WaterHCID 962—
溶媒Ethyl AcetateHCID 8857—
溶媒1,4-DioxaneHCID 31275—
生成物HCID 178456859HCID 178456859—

反応条件

温度100 °C

反応手順

To a mixture of 3-iodo-6-methyl-2-[1-(9H-purin-6-ylamino)propyl]-4H-pyrido[1,2-a]pyrimidin-4-one (0.030 g, 0.065 mmol) and (5-fluoropyridin-3-yl)boronic acid (Combi-Blocks, 11.0 mg, 0.0780 mmol) in 1,4-dioxane (0.5 mL) was added a 1 M solution of sodium carbonate (8.27 mg, 0.0780 mmol) in water (0.077 mL) and tetrakis(triphenylphosphine)palladium (0) (3.76 mg, 0.00325 mmol). The reaction mixture was heated at 100° C. overnight. After cooling to rt, the mixture was diluted with EtOAc, washed with water, brine, dried over MgSO4, and concentrated. The residue was purified on RP-HPLC at pH 10 conditions (XBridge C18 column, eluting with a gradient of acetonitrile/water containing 0.15% NH4OH) to provide the desired product. LCMS calculated for C22H20FN8O (M+H)+: m/z=431.2. Found: 431.3.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US09434746B2
出典データセットuspto-grants-2016_09
ORD IDord-9f735ffbfdff48efa3cc3170230ded1b
出典メモuspto-grants-2016_09