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Diisopropylamine → Rac-cis-(2-(((5-chloropyrimidin-2-yl)amino)methyl)-3-methylpiperidin-1-yl)(2-(trifluoromethoxy)phenyl)methanone
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Diisopropylamine | HCID 7912 | — |
| 反応物 | 2-(Trifluoromethoxy)benzoyl Chloride | HCID 2777241 | — |
| 反応物 | rac-cis-5-chloro-N-((3-methylpiperidin-2-yl)methyl)pyrimidin-2-amine | HCID 131737160 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | Rac-cis-(2-(((5-chloropyrimidin-2-yl)amino)methyl)-3-methylpiperidin-1-yl)(2-(trifluoromethoxy)phenyl)methanone | HCID 131737159 | — |
反応手順
To a solution of the forementioned rac-cis-5-chloro-N-((3-methylpiperidin-2-yl)methyl)pyrimidin-2-amine and diisopropylamine (3 eq) in DCM was added 2-(trifluoromethoxy)benzoyl chloride (1.2 eq) dropwise. The reaction was stirred at reflux for 3 h and concentrated in vacuo. The crude reaction mixture was purified by reverse-phase preparative HPLC to afford the title compound. (ESI) 429.1 (M+H).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US09440982B2 |
| 出典データセット | uspto-grants-2016_09 |
| ORD ID | ord-eaaf1ad515e04aa992625b49ead578e7 |
| 出典メモ | uspto-grants-2016_09 |