[I:1][C:2]1[CH:7]=[CH:6][C:5]([CH2:8][C:9](=O)[CH2:10][CH3:11])=[CH:4][CH:3]=1.[BH3-]C#[N:15].[Na+]>CC(O)C>[I:1][C:2]1[CH:7]=[CH:6][C:5]([CH2:8][CH:9]([NH2:15])[CH2:10][CH3:11])=[CH:4][CH:3]=15.95 g (21.7 mmol) 1-(4-iodophenyl)-butane-2-one (I39) are added to 150 mL 2-propanol and transferred into an autoclav. 25.1 g (326 mmol) NH4OAc and 4.09 g (65.1 mmol) NaCNBH3 are added and the mixture is stirred at 90° C. over night. The reaction is quenched by the addition of sat. aq. NaHCO3 solution and extracted with EtOAc (3×). The combined organic layers are washed with brine, dried with Na2SO4 and the solvent is removed in vacuo. The compound is used without further purification.
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