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Potassium Carbonate → (R)-N-cyclopropyl-4-methyl-3-(3-(1-(2-(oxiran-2-ylmethoxy)phenyl)cyclopropylamino)-2-oxopyrazin-1(2H)-yl)benzamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Potassium Carbonate | HCID 11430 | — |
| 反応物 | Cesium fluoride | HCID 25953 | — |
| 反応物 | Benzenesulfonic acid, 3-nitro-, (2R)-2-oxiranylmethyl ester | HCID 146513 | — |
| 反応物 | HCID 66688774 | HCID 66688774 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | (R)-N-cyclopropyl-4-methyl-3-(3-(1-(2-(oxiran-2-ylmethoxy)phenyl)cyclopropylamino)-2-oxopyrazin-1(2H)-yl)benzamide | HCID 86663253 | — |
反応手順
Potassium carbonate (216 mg) and cesium fluoride (36.5 mg) were added to N-cyclopropyl-3-(3-(1-(2-hydroxyphenyl)cyclopropylamino)-2-oxopyrazin-1(2H)-yl)-4-methylbenzamide (Example 167d, 500 mg) in DMF (9 mL) and stirred for 1 h. (R)-oxiran-2-ylmethyl 3-nitrobenzenesulfonate (311 mg) was added and the reaction stirred for 3 days. The reaction mixture was used without isolation/purification.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08889692B2 |
| 出典データセット | uspto-grants-2014_11 |
| ORD ID | ord-bea578bc2d2d4900aded24217eb37849 |
| 出典メモ | uspto-grants-2014_11 |