関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Benzyl Bromide | HCID 7498 | — |
| 反応物 | 7-Chloro-6-fluoroisoquinolin-1(2H)-one | HCID 59818248 | — |
| 触媒 | HCID 178418647 | HCID 178418647 | — |
| 溶媒 | Toluene | HCID 1140 | — |
| 生成物 | 1-Benzyloxy-7-chloro-6-fluoro-isoquinoline | HCID 59818252 | 54.2% |
反応手順
14.74 g (74.6 mmol) of 7-chloro-6-fluoro-2H-isoquinolin-1-one (7) were dissolved in 150 ml of toluene. After addition of 30.86 g (111.9 mmol) of silver carbonate and 15.31 g (89.5 mmol) of benzyl bromide, the mixture was stirred at 80° C. for 3 h. After cooling down to room temperature, the reaction mixture was filtered and the filtrate was evaporated. The residue was dissolved in dichloromethane and washed with water, dried with magnesium sulfate and evaporated. Final purification by preparative HPLC gave 11.63 g of the title compound. Rt=2.51 min (Method B). Detected mass: 288.1/290.1 (M+H+).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US08742116B2 |
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| 出典データセット | uspto-grants-2014_06 |
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| ORD ID | ord-443867873dda4ba49a649b54c0bc50c0 |
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| 出典メモ | uspto-grants-2014_06 |
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