関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Diethylamine | HCID 8021 | — |
| 反応物 | 1,4-Dithiane-2,5-diol | HCID 98330 | — |
| 反応物 | p-Fluorobenzoylacetonitrile | HCID 2783172 | — |
| 溶媒 | Ethanol | HCID 702 | — |
| 生成物 | (2-Aminothiophen-3-YL)(4-fluorophenyl)methanone | HCID 11074943 | 86.2% |
反応手順
Following a procedure described in J. Med. Chem. 2002, 45, 382-389; 0.44 g (2.7 mmol) 3-(4-fluoro-phenyl)-3-oxo-propionitrile (the preparation of which is described in example 17), 0.33 g (2.15 mmol) [1,4]dithiane-2,5-diol, 0.16 ml (2.15 mmol) diethyl-amine and 5 ml ethanol were charged in a sealed tube. The reaction mixture was heated at 50° C. for 6 h. The tube was then placed in a fridge (about 4° C.) for the night, and the product was collected by filtration and dried under vacuum to afford 0.41 g (69%) (2-amino-thiophen-3-yl)-(4-fluoro-phenyl)-methanone as a light brown crystals.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US07390903B2 |
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| 出典データセット | uspto-grants-2008_06 |
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| ORD ID | ord-42962bf534a9470cb3f05f45307509c3 |
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| 出典メモ | uspto-grants-2008_06 |
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