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Triethylamine → 5-Oxo-8-propionyl-1,2,3,5-tetrahydroindolizin-6-yl trifluoromethanesulfonate
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Triethylamine | HCID 8471 | — |
| 反応物 | 1,1,1-Trifluoro-N-phenylmethanesulfonamide | HCID 68012 | — |
| 反応物 | 6-hydroxy-8-propanoyl-2,3-dihydro-1H-indolizin-5-one | HCID 66844731 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | 5-Oxo-8-propionyl-1,2,3,5-tetrahydroindolizin-6-yl trifluoromethanesulfonate | HCID 86614016 | 99% |
反応手順
To a stirred, cooled (0° C.) solution of 6-hydroxy-8-propionyl-2,3-dihydroindolizin-5-(1H)-one (1.10 g, 4.53 mmol) in CH2Cl2 (10 mL) was added Et3N. After stirring for 20 min., N-phenyltrifluoromethane sulfonamide was added in one portion. The mixture was stirred at RT for 6 h and quenched with H2O. the mixture was extracted with CH2Cl2 (3×) and the combined organic layers were dried over MgSO4, concentrated and purified by ISCO (40% EtOAc/Hexanes) to give the title compound as a white solid (1.50 g, 99%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08163766B2 |
| 出典データセット | uspto-grants-2012_04 |
| ORD ID | ord-d0d80e3076fc4e4dba730110203e46f9 |
| 出典メモ | uspto-grants-2012_04 |