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Water → 4-[((1R)-1-{3-[(3-fluoro-4-methoxybenzoyl)amino]phenyl}ethyl)amino]quinazoline-8-carboxamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Water | HCID 962 | — |
| 反応物 | 3-Fluoro-4-methoxybenzoyl chloride | HCID 2779255 | — |
| 反応物 | 4-{[(1R)-1-(3-aminophenyl)ethyl]amino}quinazoline-8-carboxamide | HCID 66762892 | — |
| 溶媒 | Pyridine | HCID 1049 | — |
| 生成物 | 4-[((1R)-1-{3-[(3-fluoro-4-methoxybenzoyl)amino]phenyl}ethyl)amino]quinazoline-8-carboxamide | HCID 66762311 | 98% |
反応手順
A suspension of 4-{[(1R)-1-(3-aminophenyl)ethyl]amino}quinazoline-8-carboxamide (2.0 g, 6.51 mmol) in dry pyridine (50 mL) was treated with 3-fluoro-4-methoxybenzoyl chloride (1.51 g, 8.01 mmol, 1.23 eq), and the contents were stirred at room temp for 45 min. The clear-yellow solution was slowly added to water (1000 mL), and the white precipitate was filtered, washed with water (300 mL) and dried under vacuum at 35° C. to get the title compound in 98% yield (2.93 g).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08637532B2 |
| 出典データセット | uspto-grants-2014_01 |
| ORD ID | ord-92f88f09e23b483db9ea94bf56d9b571 |
| 出典メモ | uspto-grants-2014_01 |