化工社化工社 化学情報印刷レポート · 研究参考用
Paclitaxel → Fmoc-Leu PABC Paclitaxel
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Paclitaxel | HCID 36314 | — |
| 反応物 | Fmoc-Leu PABC | HCID 131731174 | — |
| 触媒 | 4-(Dimethylamino)pyridine | HCID 14284 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | Fmoc-Leu PABC Paclitaxel | HCID 131731173 | 93% |
反応手順
Paclitaxel (0.37 g, 0.44 mmol) and 4-Dimethylaminopyridine (DMAP) (0.05 g, 0.44 mmol) were added to a solution of 7 (0.27 g, 0.44 mmol) in anhydrous DCM (15 mL), and the reaction was stirred in the dark at room temperature for 24 hours. Subsequently, DCM (20 mL) was added and the reaction mixture was extracted with NaHCO3, brine and dried over sodium sulphate. The residue was purified on a silica gel column using ethyl acetate/hexane (1:1) to afford 8 (550 mg, 93%) as a white powder. ESI-MS (5 kV, MeOH): m/z (%)=1360.1 (100) [M+Na]+; HPLC (230 nm): >95%.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08642555B2 |
| 出典データセット | uspto-grants-2014_02 |
| ORD ID | ord-baa64055c72c46edb4b6fb547eebad34 |
| 出典メモ | uspto-grants-2014_02 |