関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Potassium Carbonate | HCID 11430 | — |
| 反応物 | 4-bromo-N,N-dimethylaniline | HCID 11465 | — |
| 反応物 | trans-N,N'-dimethyl-1,2-cyclohexanediamine | HCID 2733821 | — |
| 反応物 | trans-Cinnamamide | HCID 5273472 | — |
| 触媒 | Copper(1+) iodide; Copper(I) iodide; Cuprous iodide; Cuprous iodide (CuI) | HCID 24350 | — |
| 溶媒 | Toluene | HCID 1140 | — |
| 生成物 | (2E)-N-[4-(dimethylamino)phenyl]-3-phenylprop-2-enamide | HCID 728725 | 98% |
反応手順
A 15 mL resealable Schlenk tube was charged with CuI (9.6 mg, 0.0504 mmol, 5.0 mol %), 4-dimethylamino-1-bromobenzene (201 mg, 1.00 mmol), trans-cinnamamide (178 mg, 1.21 mmol), K2CO3 (280 mg, 2.03 mmol), evacuated and backfilled with argon. trans-N,N′-Dimethyl-1,2-cyclohexanediamine (16 μL, 0.102 mmol, 10 mol %) and toluene (1.0 mL) were added under argon. The Schlenk tube was sealed with a Teflon valve and the reaction mixture was stirred at 110° C. for 23 h. The resulting bright yellow suspension was allowed to reach room temperature and then filtered through a 0.5×1 cm pad of silica gel eluting with 10 mL of ethyl acetate-dichloromethane 1:1. The filtrate was concentrated, the residue was dissolved in 10 mL of dichloromethane and purified by flash chromatography on silica gel (2×20 cm, ethyl acetate-dichloromethane 1:4, 15 mL fractions). Fractions 10-20 provided 261 mg (98% yield) of the desired product as a bright yellow solid.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US06759554B2 |
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| 出典データセット | uspto-grants-2004_07 |
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| ORD ID | ord-6a66cdc9c2ab4f038d87bb3affd3e4c8 |
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| 出典メモ | uspto-grants-2004_07 |
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