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Methylamine → 2-chloro-N-methyl-7-(6-(trifluoromethyl)pyridin-3-yl)-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-amine
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Methylamine | HCID 6329 | — |
| 反応物 | 2,4-dichloro-7-(6-(trifluoromethyl)pyridin-3-yl)-6,7-dihydro-5H-cyclopenta[d]pyrimidine | HCID 58075720 | — |
| 溶媒 | N-methyl-2-pyrrolidone | HCID 13387 | — |
| 生成物 | 2-chloro-N-methyl-7-(6-(trifluoromethyl)pyridin-3-yl)-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-amine | HCID 58075615 | 24.64% |
反応手順
To a solution of 2,4-dichloro-7-(6-(trifluoromethyl)pyridin-3-yl)-6,7-dihydro-5H-cyclopenta[d]pyrimidine (33 mg, 0.099 mmol) in NMP (Volume: 5 mL) was added methanamine (0.247 mL, 0.494 mmol). The reaction mixture was stirred at room temperature for 2 h. The product was partitioned between ethyl acetate & water. The organic layers were combined and dried in vacuum to afford 2-chloro-N-methyl-7-(6-(trifluoromethyl)pyridin-3-yl)-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-amine (8 mg, 0.024 mmol, 24.64% yield). LC-MS (M+H)+=329.0.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08637525B2 |
| 出典データセット | uspto-grants-2014_01 |
| ORD ID | ord-f64355f143a343858dbb6b94e90c6337 |
| 出典メモ | uspto-grants-2014_01 |