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2-Thiophenecarbonyl chloride → Thiophene-2-carboxylic acid N-(1-Boc-piperidin-3-ylmethyl)-N-phenyl amide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 2-Thiophenecarbonyl chloride | HCID 78928 | — |
| 反応物 | N-(1-Boc-piperidin-3-ylmethyl)aniline | HCID 12972131 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | Thiophene-2-carboxylic acid N-(1-Boc-piperidin-3-ylmethyl)-N-phenyl amide | HCID 53977639 | 98% |
反応手順
To a stirred suspension of N-(1-Boc-piperidin-3-ylmethyl)-aniline 4 (60.9 mg, 0.21 mmol) and piperidinomethyl polystyrene resin (60 mg) in 0.6 mL of dry CH2Cl2 was added 2-thiophenecarbonyl chloride (97%, 39.2 mg, 1.2 eq.) at room temperature. After being shaken at room temperature for 4 hours, the reaction mixture was passed through an aminopropyl NH2 cartridge and washed with CH2Cl2. Removal of CH2Cl2 afforded thiophene-2-carboxylic acid N-(1-Boc-piperidin-3-ylmethyl)-N-phenyl amide 15 (82.1 mg, 98%). LRMS 300 (M-100)+.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US06645980B1 |
| 出典データセット | uspto-grants-2003_11 |
| ORD ID | ord-b7defdc7bdbc4aacb295c2da85bf4314 |
| 出典メモ | uspto-grants-2003_11 |