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Hydrochloric Acid → Fmoc-Val-Pro doxorubicin
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Hydrochloric Acid | HCID 313 | — |
| 反応物 | Doxorubicin | HCID 31703 | — |
| 反応物 | Diisopropylethylamine | HCID 81531 | — |
| 反応物 | Fmoc-Val-Pro-OH | HCID 54198008 | — |
| 溶媒 | Dimethyl Sulfoxide | HCID 679 | — |
| 溶媒 | Ethyl Acetate | HCID 8857 | — |
| 生成物 | Fmoc-Val-Pro doxorubicin | HCID 131729870 | 45% |
反応手順
A solution of Fmoc-Val-Pro-OH and doxorubicin. HCl (50 mg, 0.08 mmol) in DMSO (4 mL), was successively treated at room temperature with N-[(dimethylamino)1H-1,2,3-triazolo[4,5-b]pyridino-1-ylmethylene]-N-methylmethanaminium hexafluorophosphate N-oxide (HATU) (36.0 mg, 0.09 mmol) and diisopropylethylamine (DIEA) (29.5 μL, 0.17 mmol). The reaction mixture was stirred at room temperature overnight. Then, the solvent was lyophilized and the residue was dissolved in ethyl acetate and washed with citric acid (10%), NaHCO3 (10%) and brine. The organic layer was dried (Na2SO4) and evaporated to dryness to give F (45% yield).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08236756B2 |
| 出典データセット | uspto-grants-2012_08 |
| ORD ID | ord-eb975f8915e54d90b81363eb67c62aed |
| 出典メモ | uspto-grants-2012_08 |