化工社化工社 化学情報印刷レポート · 研究参考用
Cyanogen Bromide → Quinazolin-2-amine
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Cyanogen Bromide | HCID 10476 | — |
| 反応物 | Hydrate;hydrochloride | HCID 21885828 | — |
| 反応物 | ethyl-N-(6-amino-2,3-dichlorobenzyl)glycine | HCID 67080112 | — |
| 反応物 | Anagrelide | HCID 135409400 | — |
| 溶媒 | Toluene | HCID 1140 | — |
| 生成物 | Quinazolin-2-amine | HCID 178508286 | — |
反応手順
Commercially, as discussed in U.S. Pat. No. 5,801,245, and as shown in FIG. 1, anagrelide has been prepared as the hydrochloride monohydrate (compound IV) from the intermediate, ethyl-N-(6-amino-2,3-dichlorobenzyl)glycine (compound I) either by reaction with cyanogen bromide in hot alcoholic solution, or, preferentially, by reaction with cyanogen bromide in an aprotic solvent such as toluene to give the iminoquinazoline intermediate (compound II), which is isolated and then reacted with a base in a hot solution of alcohol to form anagrelide base (compound III).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08530651B2 |
| 出典データセット | uspto-grants-2013_09 |
| ORD ID | ord-16c12e29c27c4e31ace7baeccc73080c |
| 出典メモ | uspto-grants-2013_09 |