化工社化工社 化学情報印刷レポート · 研究参考用
Formamide → Quinazoline
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Formamide | HCID 713 | — |
| 反応物 | Sodium Dithionite | HCID 24489 | — |
| 反応物 | 4-(3-Chloropropyl)morpholine | HCID 95834 | — |
| 反応物 | Gefitinib | HCID 123631 | — |
| 反応物 | 3-Hydroxy-4-methoxybenzonitrile | HCID 4912822 | — |
| 生成物 | Quinazoline | HCID 9210 | — |
反応手順
WO 2004/024703 discloses a process for the preparation of gefitinib starting from 3-hydroxy-4-methoxy benzonitrile which involves condensation of 3-hydroxy-4-methoxy benzonitrile with morpholino propyl chloride, nitration, reduction with sodium dithionite to amino compound, hydrolysis of nitrile to amide, cyclisation in the presence of formamide to obtain quinazoline, chlorination with phosphorous oxychloride and finally condensation with chloro-fluoro aniline to obtain gefitinib. The process involves multiple steps and hence is time consuming.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08350029B2 |
| 出典データセット | uspto-grants-2013_01 |
| ORD ID | ord-03eb032aa21040a8a01c2c7707c6ff57 |
| 出典メモ | uspto-grants-2013_01 |