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HRID 533473作成日：2026年10月26日
4-Chloro-2-(methylthio)pyrimidine-5-carboxylic acid ethyl ester → Ethyl 2-(methylthio)-4-(1-phenylcyclopropylamino)pyrimidine-5-carboxylate
https://huagongshe.com/reaction/533473
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | 4-Chloro-2-(methylthio)pyrimidine-5-carboxylic acid ethyl ester | HCID 80008 | — |
| 反応物 | Diisopropylethylamine | HCID 81531 | — |
| 反応物 | 1-Phenyl-cyclopropylamine | HCID 194549 | — |
| 溶媒 | Acetonitrile | HCID 6342 | — |
| 溶媒 | Ethyl Acetate | HCID 8857 | — |
| 生成物 | Ethyl 2-(methylthio)-4-(1-phenylcyclopropylamino)pyrimidine-5-carboxylate | HCID 58098733 | 104.2% |
反応手順
To a solution of ethyl 4-chloro-2-(methylthio)pyrimidine-5-carboxylate (550 mg, 2.36 mmol) and 1-phenylcyclopropanamine (420 mg, 3.16 mmol) in CH3CN (6 mL) at room temperature was added DIEA (0.5 mL, 2.60 mmol). The mixture was stirred at room temperature for 3 h and 50° C. for 3 h. The mixture was diluted with EtOAc, washed with 1N HCl, Sat. NaHCO3, brine, dried and concentrated to give ethyl 2-(methylthio)-4-(1-phenylcyclopropylamino)pyrimidine-5-carboxylate (810 mg).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US08853230B2 |
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| 出典データセット | uspto-grants-2014_10 |
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| ORD ID | ord-1f5f0e7ef35740929a7bdd0dedca2103 |
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| 出典メモ | uspto-grants-2014_10 |
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