HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
Hydrochloric Acid → Fmoc-Val-Pro doxorubicin
Beteiligte Stoffe
| Rolle | Name | HCID | Einwaage |
|---|---|---|---|
| Edukt | Hydrochloric Acid | HCID 313 | — |
| Edukt | Doxorubicin | HCID 31703 | — |
| Edukt | Diisopropylethylamine | HCID 81531 | — |
| Edukt | Fmoc-Val-Pro-OH | HCID 54198008 | — |
| Lösungsmittel | Dimethyl Sulfoxide | HCID 679 | — |
| Lösungsmittel | Ethyl Acetate | HCID 8857 | — |
| Produkt | Fmoc-Val-Pro doxorubicin | HCID 131729870 | 45% |
Reaktionsschritte
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).
Herkunft & Nachweise
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patentnummer | US08236756B2 |
| Quelldatensatz | uspto-grants-2012_08 |
| ORD ID | ord-eb975f8915e54d90b81363eb67c62aed |
| Quellennotiz | uspto-grants-2012_08 |