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4-Methylmorpholine → N-(2-Amino-Pyrimidin-5-yl)-2-Chloro-5-(3-Trifluoromethyl-Benzoylamino)-Benzamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 4-Methylmorpholine | HCID 7972 | — |
| 反応物 | Pyrimidine-2,5-diamine | HCID 229075 | — |
| 反応物 | 2-Chloro-5-(3-(trifluoromethyl)benzamido)benzoic acid | HCID 53401172 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | N-(2-Amino-Pyrimidin-5-yl)-2-Chloro-5-(3-Trifluoromethyl-Benzoylamino)-Benzamide | HCID 24962185 | 73% |
反応手順
A solution of intermediate 1 (Example 2) (380 mg, 1.11 mmol) in DCM was charged with CDMT (233 mg, 1.33 mmol), and NMM (0.3 mL, 2.73 mmol). After 1 hr of stirring, 2,5-diaminopyrimidine (121 mg, 1.10 mmol) was added and the solution was allowed to stir for 48 h. The mixture was concentrated and purified by HPLC to afford the title compound as a white solid (350 mg, 73%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08030487B2 |
| 出典データセット | uspto-grants-2011_10 |
| ORD ID | ord-22c9db19a4fe4ff899c5f9e817647a15 |
| 出典メモ | uspto-grants-2011_10 |