HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
Potassium Phosphate, Tribasic → 2-(4-(dimethoxymethyl)pyridin-3-yl)-7-(trifluoromethyl)-3,4-dihydroisoquinolin-1(2H)-one
Beteiligte Stoffe
| Rolle | Name | HCID | Einwaage |
|---|---|---|---|
| Edukt | Potassium Phosphate, Tribasic | HCID 62657 | — |
| Edukt | 3-Bromo-4-(dimethoxymethyl)pyridine | HCID 20715145 | — |
| Edukt | 7-(Trifluoromethyl)-3,4-dihydroisoquinolin-1(2H)-one | HCID 66801593 | — |
| Katalysator | Copper iodide | HCID 83717 | — |
| Lösungsmittel | 1,4-Dioxane | HCID 31275 | — |
| Produkt | 2-(4-(dimethoxymethyl)pyridin-3-yl)-7-(trifluoromethyl)-3,4-dihydroisoquinolin-1(2H)-one | HCID 66803558 | 98,8% |
Reaktionsschritte
Using analogous conditions as described for the preparation of Example 1A above, 7-trifluoromethyl-3,4-dihydro-2H-isoquinolin-1-one (I-4-d: 505.4 mg, 2.3503 mmol) was reacted with 3-Bromo-4-dimethoxymethyl-pyridine (I-52a: 600 mg, 2.5854 mmol), 1,4-dioxane (20 mL), copper iodide (44.6 mg, 0.2348 mmol), trans-N,N′-dimethyl-cyclohexyl-1,2-diamine (80.9 mg, 0.7052 mmol) and potassium phosphate (1.49 g, 7.0507 mmol) to afford the crude product. Purification by column chromatography on silica gel (1% methanol in CHCl3) afforded 850 mg of the product (98.8% yield).
Herkunft & Nachweise
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patentnummer | US08946260B2 |
| Quelldatensatz | uspto-grants-2015_02 |
| ORD ID | ord-6f259627d6cd48959c39072f4dc87b60 |
| Quellennotiz | uspto-grants-2015_02 |