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2-(3-Benzyloxypyridin-4-yl)-5-(trifluoromethyl)benzoxazole → 4-[5-(Trifluoromethyl)benzoxazole-2-yl]pyridin-3-ol
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 2-(3-Benzyloxypyridin-4-yl)-5-(trifluoromethyl)benzoxazole | HCID 66880113 | — |
| 反応物 | HCID 178418361 | HCID 178418361 | — |
| 触媒 | Palladium | HCID 23938 | — |
| 溶媒 | Acetic Acid | HCID 176 | — |
| 生成物 | 4-[5-(Trifluoromethyl)benzoxazole-2-yl]pyridin-3-ol | HCID 136331268 | 96.9% |
反応手順
A mixture of 4.69 g of 2-(3-benzyloxypyridin-4-yl)-5-(trifluoromethyl)benzoxazole, 1.0 g of 5% palladium on carbon and 70 ml of acetic acid was stirred under about one atmosphere of hydrogen at room temperature for nine hours. The reaction mixture was filtered through Celite™. The filtrate was concentrated under reduced pressure. The residue was subjected to silica gel column chromatography to give 3.44 g of 4-[5-(trifluoromethyl)benzoxazole-2-yl]pyridin-3-ol (hereinafter, referred to as “active compound 114”).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08609705B2 |
| 出典データセット | uspto-grants-2013_12 |
| ORD ID | ord-29f354b790744125810ef24e65783a20 |
| 出典メモ | uspto-grants-2013_12 |