HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
1,2-Diaminocyclohexane, trans- → 7-Trifluoromethyl-2-(4-trifluoromethyl-pyridin-3-yl)-3,4-dihydro-2H-isoquinolin-1-one
Beteiligte Stoffe
| Rolle | Name | HCID | Einwaage |
|---|---|---|---|
| Edukt | 1,2-Diaminocyclohexane, trans- | HCID 43806 | — |
| Edukt | Potassium Phosphate, Tribasic | HCID 62657 | — |
| Edukt | 3-Bromo-4-(trifluoromethyl)pyridine | HCID 19937263 | — |
| Edukt | 7-(Trifluoromethyl)-3,4-dihydroisoquinolin-1(2H)-one | HCID 66801593 | — |
| Katalysator | Copper iodide | HCID 83717 | — |
| Lösungsmittel | 1,4-Dioxane | HCID 31275 | — |
| Produkt | 7-Trifluoromethyl-2-(4-trifluoromethyl-pyridin-3-yl)-3,4-dihydro-2H-isoquinolin-1-one | HCID 56942890 | 6,5% |
Reaktionsschritte
Using analogous reaction conditions as described in Example 1, 7-trifluoromethyl-3,4-dihydro-2H-isoquinolin-1-one (I-16c: 150 mg, 0.684 mmol) was reacted with 3-bromo-4-trifluoromethyl-pyridine (154.7 mg, 0.684 mmol), 1,4-dioxane (5 mL), copper iodide (12.96 mg, 0.0684 mmol), trans-1,2-diamino cyclohexane (23.39 mg, 0.2084 mmol) and potassium phosphate (434.6 mg, 2.05 mmol) to afford the crude product. Purification by preparative HPLC afforded 16 mg of the product (6.5% yield).
Herkunft & Nachweise
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patentnummer | US08946260B2 |
| Quelldatensatz | uspto-grants-2015_02 |
| ORD ID | ord-90bd680009bf4821b311c019b71ece13 |
| Quellennotiz | uspto-grants-2015_02 |