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5-{2-[2-(Acetylamino)-1,3-thiazol-4-yl]vinyl}thiophene-2-carboxylic acid → 5-{2-[2-(Acetylamino)-1,3-thiazol-4-yl]ethyl}thiophene-2-carboxylic acid
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 5-{2-[2-(Acetylamino)-1,3-thiazol-4-yl]vinyl}thiophene-2-carboxylic acid | HCID 86650005 | — |
| 触媒 | HCID 178418390 | HCID 178418390 | — |
| 溶媒 | Methanol | HCID 887 | — |
| 溶媒 | Tetrahydrofuran | HCID 8028 | — |
| 生成物 | 5-{2-[2-(Acetylamino)-1,3-thiazol-4-yl]ethyl}thiophene-2-carboxylic acid | HCID 86650006 | 81.4% |
反応手順
5-{2-[2-(Acetylamino)-1,3-thiazol-4-yl]vinyl}thiophene-2-carboxylic acid (900.0 mg, 3.058 mmol) was dissolved in a mixed solvent of tetrahydrofuran (250 ml) and methanol (100 ml). 20% Palladium carbon was added, and the mixture was hydrogenated at room temperature under 4 atm. After the completion of the reaction, the reaction mixture was filtered through celite, and the filtrate was concentrated under reduced pressure. Diethyl ether (100 ml) was added to the concentrated residue, and the precipitate was collected by filtration, washed with diethyl ether, and dried under reduced pressure to give 5-{2-[2-(acetylamino)-1,3-thiazol-4-yl]ethyl}thiophene-2-carboxylic acid (738.1 mg, 2.490 mmol, yield 81.4%) as an off-white solid.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08507690B2 |
| 出典データセット | uspto-grants-2013_08 |
| ORD ID | ord-6c950cf75ba840c38818ccc0ebcef983 |
| 出典メモ | uspto-grants-2013_08 |