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4,6-Dichloro-5-(2-methoxyphenoxy)-2-(pyridin-4-YL)pyrimidine → 2-Phenyl-ethanesulfonic acid [6-chloro-5-(2-methoxy-phenoxy)-2-pyridin-4-yl-pyrimidin-4-yl]-amide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 4,6-Dichloro-5-(2-methoxyphenoxy)-2-(pyridin-4-YL)pyrimidine | HCID 11175458 | — |
| 反応物 | 2-Phenyl-ethanesulfonic acid amide potassium salt | HCID 68898150 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | 2-Phenyl-ethanesulfonic acid [6-chloro-5-(2-methoxy-phenoxy)-2-pyridin-4-yl-pyrimidin-4-yl]-amide | HCID 86592471 | 78.1% |
反応手順
A solution of 4,6-dichloro-5-(2-methoxyphenoxy)-2-(4-pyridyl)-pyrimidine (2 g) and 2-phenyl-ethanesulfonic acid amide potassium salt (2.82 g, Referential Example 1e) in DMF (50 ml) was stirred at rt for 16 h. Bulk of the solvent was evaporated before it was diluted with diethyl ether (50 ml). The mixture was acidified with 10% aq. citric acid. The precipitate that formed was collected, washed with diethyl ether (100 ml) and dried to give 2-phenyl-ethanesulfonic acid [6-chloro-5-(2-methoxy-phenoxy)-2-pyridin-4-yl-pyrimidin-4-yl]-amide (2.23 g) as a beige powder. LC-MS: tR=4.93 min, [M+1]+=497.22, [M−1]−=494.96.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07091201B2 |
| 出典データセット | uspto-grants-2006_08 |
| ORD ID | ord-50ab374672784712afdda58eb7ef9ef4 |
| 出典メモ | uspto-grants-2006_08 |