化工社化工社 化学情報印刷レポート · 研究参考用
Acetic Acid → 4-Methanesulfonyloxy-5-methoxy-7-[1-(tert-butoxycarbonyl)-5-(cyclopropylaminomethyl)indol-2-yl]isoindolinone
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Acetic Acid | HCID 176 | — |
| 反応物 | Cyclopropylamine | HCID 69828 | — |
| 反応物 | Sodium triacetoxyborohydride | HCID 5049666 | — |
| 反応物 | 4-Methanesulfonyloxy-5-methoxy-7-[1-(tert-butoxycarbonyl)-5-formylindol-2-yl]isoindolinone | HCID 86628301 | — |
| 溶媒 | Acetonitrile | HCID 6342 | — |
| 生成物 | 4-Methanesulfonyloxy-5-methoxy-7-[1-(tert-butoxycarbonyl)-5-(cyclopropylaminomethyl)indol-2-yl]isoindolinone | HCID 86628300 | 72.2% |
反応手順
In a similar manner to Step 2 of Example 6, 4-methanesulfonyloxy-5-methoxy-7-[1-(tert-butoxycarbonyl)-5-formylindol-2-yl]isoindolinone (50 mg, 0.100 mmol) was dissolved in acetonitrile (2.9 mL), and the solution was treated with cyclopropylamine (0.069 mL, 1.0 mmol), acetic acid (0.115 mL, 2.00 mmol) and sodium triacetoxyborohydride (64 mg, 0.30 mmol) to obtain 4-methanesulfonyloxy-5-methoxy-7-[1-(tert-butoxycarbonyl)-5-(cyclopropylaminomethyl)indol-2-yl]isoindolinone (39.1 mg, yield 72%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07745641B2 |
| 出典データセット | uspto-grants-2010_06 |
| ORD ID | ord-fddd7ad5565f4e5085576bd82ab16ad9 |
| 出典メモ | uspto-grants-2010_06 |