HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
Triphenylphosphine → 3-(3,5-difluorophenyl)-6-(3-(4-methylpiperazin-1-yl)propoxy)-2-(pyridin-3-yl)-1H-inden-1-one
Beteiligte Stoffe
| Rolle | Name | HCID | Einwaage |
|---|---|---|---|
| Edukt | Triphenylphosphine | HCID 11776 | — |
| Edukt | Diisopropyl azodicarboxylate | HCID 5363146 | — |
| Edukt | t-Butyl 3-(4-methylpiperazin-1-yl)propan-1-ol | HCID 62623028 | — |
| Edukt | 2-bromo-6-hydroxy-3-phenyl-1H-inden-1-one | HCID 70306176 | — |
| Edukt | 3-(3,5-difluorophenyl)-6-hydroxy-2-(pyridin-3-yl)-1H-inden-1-one | HCID 70317432 | — |
| Produkt | 3-(3,5-difluorophenyl)-6-(3-(4-methylpiperazin-1-yl)propoxy)-2-(pyridin-3-yl)-1H-inden-1-one | HCID 70312986 | — |
Reaktionsschritte
The procedure of Step 6 of Example 1 was repeated except for using 3-(3,5-difluorophenyl)-6-hydroxy-2-(pyridin-3-yl)-1H-inden-1-one obtained in Step 1 of Example 64 as a starting material instead of 2-bromo-6-hydroxy-3-phenyl-1H-inden-1-one, t-butyl 3-(4-methylpiperazin-1-yl)propan-1-ol (2.0 eq) instead of 4-(2-hydroxyethyl)morpholine, using 2 equivalents of PPh3 and DIAD, being stirred for 34 h, and being purified by prep. HPLC (20% H2O/CH3CN) to provide 3-(3,5-difluorophenyl)-6-(3-(4-methylpiperazin-1-yl)propoxy)-2-(pyridin-3-yl)-1H-inden-1-one, which was treated with HCl/dioxane following the same procedure in Step 8 of Example 1 (50% for 2 steps).
Herkunft & Nachweise
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patentnummer | US08877747B2 |
| Quelldatensatz | uspto-grants-2014_11 |
| ORD ID | ord-e3a3c9261ae948a9aea7544cfb7aef91 |
| Quellennotiz | uspto-grants-2014_11 |