関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Potassium Carbonate | HCID 11430 | — |
| 反応物 | 2-methyl-1H-indol-5-ol | HCID 83336 | — |
| 反応物 | 4-Chloro-6-methoxy-7-(3-(piperidin-1-YL)propoxy)quinazoline | HCID 11002191 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | 6-Methoxy-4-(2-methylindol-5-yloxy)-7-(3-piperidinopropoxy)quinazoline | HCID 22030540 | 54.8% |
反応手順
A solution of 4-chloro-6-methoxy-7-(3-piperidinopropoxy)quinazoline (100 mg, 0.29 mmol), 5-hydroxy-2-methylindole (53 mg, 0.36 mmol), (prepared as described for the starting material in Example 48), and potassium carbonate (62 mg, 0.44 mmol) in DMF (2 ml) was heated at 85° C. for 3 hours, followed by heating at 95° C. for 2 hours. After cooling, ice/water (15 ml) was added and the precipitate was collected by filtration and dried under vacuum. The solid was purified by column chromatography eluting with methylene chloride/methanol (95/5) followed by methylene chloride/methanol/3M ammonia in methanol (95/3/2) to give 6-methoxy-4-(2-methylindol-5-yloxy)-7-(3-piperidinopropoxy)quinazoline (71 mg, 54%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US08492560B2 |
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| 出典データセット | uspto-grants-2013_07 |
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| ORD ID | ord-4cda509b26934e589b358b50bdc162a4 |
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| 出典メモ | uspto-grants-2013_07 |
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