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3-Cyanomethylphenylboronic acid → (3-{4-Chloro-3-[3,3,3-trifluoro-2-hydroxy-1-methyl-2-(4-methyl-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-6-yl)-propyl]-phenoxy}-phenyl)-acetonitrile
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 3-Cyanomethylphenylboronic acid | HCID 2773344 | — |
| 反応物 | 6-[2-(2-Chloro-5-hydroxy-phenyl)-1-hydroxy-1-trifluoromethyl-propyl]-4-methyl-4H-benzo[1,4]oxazin-3-one | HCID 66697195 | — |
| 触媒 | Cupric acetate | HCID 8895 | — |
| 溶媒 | Pyridine | HCID 1049 | — |
| 生成物 | (3-{4-Chloro-3-[3,3,3-trifluoro-2-hydroxy-1-methyl-2-(4-methyl-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-6-yl)-propyl]-phenoxy}-phenyl)-acetonitrile | HCID 66697216 | — |
反応手順
In analogy to Example 5, 6-[2-(2-chloro-5-hydroxy-phenyl)-1-hydroxy-1-trifluoromethyl-propyl]-4-methyl-4H-benzo[1,4]oxazin-3-one (Example 1, step 4) was reacted with 3-cyanomethylphenylboronic acid, copper-(II)-acetate and pyridine to give the title compound as an off-white solid. MS (m/e)=531.1 [M+H+].
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08450313B2 |
| 出典データセット | uspto-grants-2013_05 |
| ORD ID | ord-1b16daa8c84f4d2c851d72263a8ade70 |
| 出典メモ | uspto-grants-2013_05 |