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2-[5-Methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl]-1-{4-[4-(naphthalen-1-ylethynyl)-1,3-thiazol-2-yl]piperidin-1-yl}ethanone → 2-[5-methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl]-1-(4-{4-[2-(naphthalen-1-yl)ethyl]-1,3-thiazol-2-yl}piperidin-1-yl)ethanone
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 2-[5-Methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl]-1-{4-[4-(naphthalen-1-ylethynyl)-1,3-thiazol-2-yl]piperidin-1-yl}ethanone | HCID 67156152 | — |
| 触媒 | Ammonium formate | HCID 2723923 | — |
| 触媒 | Palladium hydroxide | HCID 9942167 | — |
| 溶媒 | Methanol | HCID 887 | — |
| 生成物 | 2-[5-methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl]-1-(4-{4-[2-(naphthalen-1-yl)ethyl]-1,3-thiazol-2-yl}piperidin-1-yl)ethanone | HCID 67156662 | 54.3% |
反応手順
2-[5-Methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl]-1-{4-[4-(naphthalen-1-ylethynyl)-1,3-thiazol-2-yl]piperidin-1-yl}ethanone (I-50, 157 mg) is dissolved in methanol (1.5 ml) and, at 60° C., reacted with ammonium formiate (195 mg) and 20% Pd(OH)2/C (4 mg) as catalyst. The catalyst is filtered off and the solvent is removed under reduced pressure, giving 2-[5-methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl]-1-(4-{4-[2-(naphthalen-1-yl)ethyl]-1,3-thiazol-2-yl}piperidin-1-yl)ethanone (86 mg) as a colourless oil.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07943774B2 |
| 出典データセット | uspto-grants-2011_05 |
| ORD ID | ord-a22797a269504ad98967f5edf45ce244 |
| 出典メモ | uspto-grants-2011_05 |