Ammonia → HCID 68592703, compound

Participants

Reaction Conditions

Reaction Steps

0.32 mL (2.5 mmol) chloro-trimethyl-silane were added to a suspension of 450 mg (0.84 mmol) (R)-3-(4-amino-3-chloro-5-trifluoromethyl-phenyl)-2-benzyloxy-1-[4-(4-methyl-piperazin-1-yl)-piperidin-1-yl]-propan-1-one and 380 mg (2.5 mmol) NaI in 30 mL acetonitrile and the reaction mixture was stirred for 7 h at 80° C. 30 mL EtOH and 20 mL isopropanol were added, the mixture was stirred for 30 min at RT, 15 mL of NH3 solution were added and the mixture was stirred for a further 30 min. It was evaporated down i. vac., the residue was combined with 100 mL 15% K2CO3 solution, extracted with 100 mL EtOAc, the organic phase was separated off, washed with 3% Na2SO3 solution and trocknete over Na2SO4. After the desiccant and solvent had been eliminated the residue was further reacted without purification.

Provenance & Evidence