関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Water | HCID 962 | — |
| 反応物 | Cesium carbonate | HCID 10796 | — |
| 反応物 | 2,4-Difluoropyridine | HCID 2762838 | — |
| 反応物 | (S)-N-{1-[4-(3-Hydroxy-azetidin-1-yl)-phenyl]ethyl}-acetamide | HCID 86689005 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | (S)-N-(1-{4-[3-(2-Fluoro-pyridin-4-yloxy)-azetidin-1-yl]-phenyl}-ethyl)-acetamide | HCID 86689013 | — |
反応手順
1.0 g (4.3 mmol) (S)—N-{1-[4-(3-Hydroxy-azetidin-1-yl)-phenyl]-ethyl}-acetamide (V.1), 0.6 g (5.2 mmol) 2,4-difluoropyridine and 2.0 g (6.2 mmol) cesium carbonate are combined in 40 mL DMF and the mixture is stirred for 12 h at 80° C. Water is added and the mixture is extracted twice with ethylacetate. After concentration in vacuo the residue is purified by chromatography (silica; ethylacetate) to yield the desired product.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 特許番号 | US08530461B2 |
|---|
| 出典データセット | uspto-grants-2013_09 |
|---|
| ORD ID | ord-85a0c2d0eaa043fabddad6d68fafa6c6 |
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| 出典メモ | uspto-grants-2013_09 |
|---|
