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Dimethylformamide → N-(4-Methoxybenzyl) 4-amino-2-methylmercaptopyrimidine-5-carboxyamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Dimethylformamide | HCID 6228 | — |
| 反応物 | 4-Methoxybenzylamine | HCID 75452 | — |
| 反応物 | 1-Hydroxybenzotriazole | HCID 75771 | — |
| 反応物 | 4-Amino-2-(methylthio)pyrimidine-5-carboxylic acid | HCID 22134738 | — |
| 生成物 | N-(4-Methoxybenzyl) 4-amino-2-methylmercaptopyrimidine-5-carboxyamide | HCID 131728064 | 81% |
反応手順
To a solution of 4-amino-2-methylmercaptopyrimidine-5-carboxylic acid (185 mg, 1 mmol) and p-methoxybenzyl amine (164 mg, 1.2 mmol) in N,N-dimethylformamide was added 1-hydroxybenzotriazole (92 mg, 92 mmol) and 1-(3-dimethylaminopropyl)-3-ethylcarboiimide hydrochloride (229 mg, 1.2 mmol). The reaction mixture was stirred at room temperature over night. The solvent was removed under reduce pressure. The residue was dissolved in ethyl acetate (30 mL) and washed by water (30 mL) and brine (30 mL), dried over sodium sulfate, and the solvent was ecaporated. The residue was purified by column chromatography (hexanes:ethyl acetate=1:1) to give the desired product as a white powder (245 mg, 81%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07700622B2 |
| 出典データセット | uspto-grants-2010_04 |
| ORD ID | ord-598e6ff58c9f4a9f9c8143bed7451642 |
| 出典メモ | uspto-grants-2010_04 |