関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Cesium carbonate | HCID 10796 | — |
| 反応物 | tert-Butyl bromoacetate | HCID 79177 | — |
| 反応物 | 2-cyclopropyl-4-(trifluoromethyl)-1H-indole-5-carbonitrile | HCID 67404472 | — |
| 溶媒 | Acetonitrile | HCID 6342 | — |
| 生成物 | 1,1-Dimethylethyl [5-cyano-2-cyclopropyl-4-(trifluoromethyl)-1H-indol-1-yl]acetate | HCID 71108666 | 84.4% |
反応手順
To a solution of 2-cyclopropyl-4-(trifluoromethyl)-1H-indole-5-carbonitrile (Example 165A) (1.0 g, 4.0 mmol) in dry acetonitrile (25 mL) was added cesium carbonate (2.6 g, 8.0 mmol) and t-butyl bromoacetate (768 uL, 5.2 mmol) at rt. The mixture was stirred at 85° C. overnight. The solid was filtered and the filtrate was then concentrated in vacuo. The residue was triturated with EtOAc-hexane to afford the title compound (1.23 g) in quantitative yield: MS (ES) m/z 365 (M+1).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 特許番号 | US08673948B2 |
|---|
| 出典データセット | uspto-grants-2014_03 |
|---|
| ORD ID | ord-5b0950a84b024c7ebc3f5a8cd594b15c |
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| 出典メモ | uspto-grants-2014_03 |
|---|
