関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Triethylamine | HCID 8471 | — |
| 反応物 | Benzene, 1-iodo-2-(trifluoromethyl)- | HCID 67957 | — |
| 反応物 | N-(3-ethynylphenyl)-4-hydroxy-3-methoxyphenyacetamide | HCID 86760178 | — |
| 触媒 | Copper(1+) iodide; Copper(I) iodide; Cuprous iodide; Cuprous iodide (CuI) | HCID 24350 | — |
| 触媒 | HCID 178419050 | HCID 178419050 | — |
| 溶媒 | Acetonitrile | HCID 6342 | — |
| 生成物 | 4-Hydroxy-3-methoxy-n-[3-[2-(2-trifluoromethylphenyl)ethynyl]phenyl]phenylacetamide | HCID 12096663 | — |
反応手順
A mixture of N-(3-ethynylphenyl)-4-hydroxy-3-methoxypheny-acetamide (the compound of Example 19) (200 mg), 1-trifluoromethyl-2-iodobenzene (280 mg), copper (I) iodide (19 mg), bis(triphenylphosphine)palladium (II) dichloride (70 mg), triethylamine (1 g) and acetonitrile (3 ml) is heated with stirring at 50° C. under argon atmosphere for 18 hours. The solvent is evaporated under reduced pressure, and the residue is purified by silica gel column chromatography (eluent: gradient from 0% to 100% hexane/ethyl acetate) to give the desired compound (120 mg).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 特許番号 | US07084176B2 |
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| 出典データセット | uspto-grants-2006_08 |
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| ORD ID | ord-b5a3ba4d153e4ab996f6b3ba98b5134c |
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| 出典メモ | uspto-grants-2006_08 |
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