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HRID 535353作成日:2026年10月25日

2,3-Dichloropyridine → 6-(3-Chloropyridin-2-yl)-N-(6-(trifluoromethyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-amine

https://huagongshe.com/reaction/535353

反応式

関与物質

役割名称HCID仕込み量
反応物2,3-DichloropyridineHCID 16988—
反応物DiisopropylethylamineHCID 81531—
反応物N-(6-(Trifluoromethyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-amineHCID 59346451—
溶媒dioxane N,N-dimethylacetamideHCID 67000103—
生成物6-(3-Chloropyridin-2-yl)-N-(6-(trifluoromethyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-amineHCID 5934654128%

反応条件

温度150 °C

反応手順

N-(6-(Trifluoromethyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-amine (130 mg, 0.44 mmol) was dissolved in a mixture of dioxane/N,N-dimethylacetamide (4:1) (2 mL). To the mixture was added 2,3-dichloropyridine (98 mg, 0.66 mmol) and N,N-diisopropylethylamine (0.11 mL, 0.66 mmol). The mixture was heated at 150° C. in a Personal Chemistry microwave for 16 h. The solvents were removed under vacuum and the residue was dissolved in ethyl acetate and washed with sat. NaHCO3 and brine. The organic layer was dried over Na2SO4, filtered and evaporated to give a brown residue. The residue was purified using a gradient of ethyl acetate:hexane (0-100%) to give the desired compound as an off-white powder (50 mg, 28%).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08859545B2
出典データセットuspto-grants-2014_10
ORD IDord-ca1bc9473e8e42aab5f96955a9aded9a
出典メモuspto-grants-2014_10