関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Triethylamine | HCID 8471 | — |
| 反応物 | Tetrahydro-2-furancarbonyl chloride | HCID 551254 | — |
| 反応物 | 2-(1-Piperazinyl)-4-amino-6,7-dimethoxyquinazoline | HCID 616267 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | Terazosin | HCID 5401 | 154.9% |
反応手順
37.6 g 4-amino-2-(1-piperazinyl)-6,7-dimethoxyquinazoline and 15.8 g triethylamine are suspended in 400 ml methylene chloride. The suspension is cooled to -5° C. This suspension is stirred while 21.0 g tetrahydrofuran-2-carboxylic acid chloride are added drop by drop. The suspension is continued to be stirred for two hours at 0° C., thereafter the solvent is distilled off under vacuum. 200 ml methanol and 200 ml acetone are added to the residue. The resulting suspension is kept under reflux for 0.5 hours while stirring. Thereafter, it is cooled to 0° C. The product is isolated by filtration. 78 g of moist terazosin base are obtained.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US05959108 |
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| 出典データセット | uspto-grants-1999_09 |
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| ORD ID | ord-30e79277aa3a428797898df30a3543a7 |
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| 出典メモ | uspto-grants-1999_09 |
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