p-Toluenesulfonic acid → (R)-(4-(4-(4-(2-hydroxyethyl)phenyl)phthalazin-1-yl)-3-methylpiperazin-1-yl)(phenyl)methanone

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Reaction Steps

((R)-3-methyl-4-(4-(4-(2-(tetrahydro-2H-pyran-2-yloxy)ethyl)phenyl)phthalazin-1-yl)piperazin-1-yl)(phenyl)methanone (122 mg, 0.227 mmol) 83 and p-toluenesulfonic acid (130 mg, 0.682 mmol) were dissolved in methanol (4 mL) and stirred at rt for 1.5 hours. The reaction was added to 35 mL aqueous K2CO3 (10%) and extracted three times with 30 mL portions of dichloromethane. The combined organic extracts were dried over MgSO4 and evaporated to give a pale yellow solid, compound 84. MS (M+H)+=453.2.

Provenance & Evidence