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Dichloromethane → 3-{[7-(3-chloropropoxy)-6-methoxyquinazolin-4-yl]amino}-N-(3-fluorophenyl)-1H-pyrazole-5-carboxamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Dichloromethane | HCID 6344 | — |
| 反応物 | 1,4-Dioxane | HCID 31275 | — |
| 反応物 | 4-Chloro-7-(3-chloropropoxy)-6-methoxyquinazoline | HCID 57447227 | — |
| 反応物 | 3-amino-N-(3-fluorophenyl)-1H-pyrazole-5-carboxamide | HCID 64523814 | — |
| 溶媒 | Hydrochloric Acid | HCID 313 | — |
| 溶媒 | Dimethylacetamide | HCID 31374 | — |
| 生成物 | 3-{[7-(3-chloropropoxy)-6-methoxyquinazolin-4-yl]amino}-N-(3-fluorophenyl)-1H-pyrazole-5-carboxamide | HCID 68987461 | 88% |
反応手順
3-Amino-N-(3-fluorophenyl)-1H-pyrazole-5-carboxamide (153 mg, 0.69 mmol) in dimethylacetamide (1.8 ml) and HCl in dioxane (4 M solution in dioxane, 174 μl, 0.69 mmol) was reacted with 4-chloro-7-(3-chloropropoxy)-6-methoxyquinazoline (200 mg, 0.69 mmol) at 90° C. for 1.5 hour. Dichloromethane (35 ml) was added to the cooled reaction mixture, and the solid recovered by filtration, washed with dichloromethane and dried to yield 3-{[7-(3-chloropropoxy)-6-methoxyquinazolin-4-yl]amino}-N-(3-fluorophenyl)-1H-pyrazole-5-carboxamide (286 mg, 81% yield):
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07402585B2 |
| 出典データセット | uspto-grants-2008_07 |
| ORD ID | ord-4dc25890c54c435fb884c5cabd4bf5ab |
| 出典メモ | uspto-grants-2008_07 |