Cesium carbonate → 6-{4-[4-(5-Chloro-1H-indole-2-sulfonyl)-2-oxo-piperazin-1-ylmethyl]-phenyl}-2-(2-morpholin-4-yl-ethyl)-2H-pyridazin-3-one

Beteiligte Stoffe

Reaktionsbedingungen

Reaktionsschritte

6-Chloro-2-(2-morpholin-4-yl-ethyl)-2H-pyridazin-3-one hydrochloride, (63 mg, 0.22 mmol), 4-({4-[(5-chloro-1H-indol-2-yl)sulphonyl]piperazin-1-yl}carbonyl)-phenyl boronic acid (78 mg, 0.17 mmol), caesium carbonate (156 mg, 0.48 mmol), and bis(triphenylphosphine) palladium (II) chloride (11 mg, 0.02 mmol,) were mixed in 2.0 mL of dimethyl acetamide/water/ethanol; 7:3:2) in a microwave vial. The reaction was heated to 150° C. for 150 seconds. After cooling, the mixture was filtered and loaded onto a reversed-phase preparative HPLC for purification. After freezing dry of pooled fractions, 71 mg (67%) of the product was obtained as a white powder.

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