Reaktion #41938

Reaktionsgleichung

6-Bromo-3-methanesulfonyl-2-methyl-4-morpholin-4-yl-quinoline

compound

6-Bromo-3-methanesulfonyl-2-methyl-4-morpholin-4-yl-quinoline

trans-2-phenylcyclopropylboronic acid

potassium phosphate

→

white crystals

Ausbeute 61.3%

3-Methanesulfonyl-2-methyl-4-morpholin-4-yl-6-((1R,2R)-2-phenyl-cyclopropyl)-quinoline

Ausbeute 61.3%

Reaktionsbedingungen

Aufarbeitung

1. 1
   Temperaturat reflux under argon for 8 h
2. 2
   SonstigeThe crude product was purified by chromatography on silica gel in dichloromethane/ethyl acetate 5:1 with a gradient from 100:0 to 80:20

Vorschrift

6-Bromo-3-methanesulfonyl-2-methyl-4-morpholin-4-yl-quinoline (compound of example 6) (300 mg, 0.78 mmol), trans-2-phenylcyclopropylboronic acid (189 mg, 1.17 mmol), potassium phosphate (496 mg, 2.33 mmol) and tetrakis(triphenylphosphine)-palladium (27 mg, 0.023 mmol) were heated at reflux under argon for 8 h. The crude product was purified by chromatography on silica gel in dichloromethane/ethyl acetate 5:1 with a gradient from 100:0 to 80:20. One obtained 202 mg (60%) of white crystals. MS: m/z=423 (M+H).

Quelle