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Potassium Carbonate → N-{1-[(3-Hydroxyazetidin-1-yl)carbonyl]-5-[4-(trifluoromethyl)phenyl]piperidin-3-yl}benzenecarboxamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Potassium Carbonate | HCID 11430 | — |
| 反応物 | 3-Hydroxyazetidine hydrochloride | HCID 2759290 | — |
| 反応物 | 4-Nitrophenyl 3-[(phenylcarbonyl)amino]-5-[4-(trifluoromethyl)phenyl]piperidine-1-carboxylate | HCID 66701467 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | N-{1-[(3-Hydroxyazetidin-1-yl)carbonyl]-5-[4-(trifluoromethyl)phenyl]piperidin-3-yl}benzenecarboxamide | HCID 66761619 | — |
反応手順
80 mg (0.16 mmol) of 4-nitrophenyl 3-[(phenylcarbonyl)amino]-5-[4-(trifluoromethyl)phenyl]piperidine-1-carboxylate were initially charged in 1.7 ml of DMF, and 51 mg (0.47 mmol) of azetidin-3-ol hydrochloride and 22 mg (0.16 mmol) of potassium carbonate were added. The mixture was reacted in a microwave (Emrys Optimizer) at 150° C. for 15 min. The crude product was then purified by preparative HPLC (Reprosil C18, water/acetonitrile gradient).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08987248B2 |
| 出典データセット | uspto-grants-2015_03 |
| ORD ID | ord-ce783993c1bb42a7bb4ea9f0cf981a5e |
| 出典メモ | uspto-grants-2015_03 |