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HRID 1843875Erstellt: 26. Oktober 2026

1,2-Diaminocyclohexane, trans- → 7-Trifluoromethyl-2-(4-trifluoromethyl-pyridin-3-yl)-3,4-dihydro-2H-isoquinolin-1-one

https://huagongshe.com/reaction/1843875

Reaktionsgleichung

Beteiligte Stoffe

RolleNameHCIDEinwaage
Edukt1,2-Diaminocyclohexane, trans-HCID 43806—
EduktPotassium Phosphate, TribasicHCID 62657—
Edukt3-Bromo-4-(trifluoromethyl)pyridineHCID 19937263—
Edukt7-(Trifluoromethyl)-3,4-dihydroisoquinolin-1(2H)-oneHCID 66801593—
KatalysatorCopper iodideHCID 83717—
Lösungsmittel1,4-DioxaneHCID 31275—
Produkt7-Trifluoromethyl-2-(4-trifluoromethyl-pyridin-3-yl)-3,4-dihydro-2H-isoquinolin-1-oneHCID 569428906,5%

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

DOI10.6084/m9.figshare.5104873.v1
PatentnummerUS08946260B2
Quelldatensatzuspto-grants-2015_02
ORD IDord-90bd680009bf4821b311c019b71ece13
Quellennotizuspto-grants-2015_02