Water → HCID 71253121, compound

Participants

Reaction Steps

(6-Amino-2-methylpyridin-3-yl)[4-(2,4-dimethylphenyl)piperazin-1-yl]methanone (180 mg) described in Preparation Example 136 and triethylamine (0.19 mL) were dissolved in dichloromethane (5 mL), 3-chloropropane-1-sulfonyl chloride (0.14 mL) was added, and the mixture was stirred at room temperature overnight. Water was added to the reaction mixture, the mixture was extracted with dichloromethane, the extract was washed with saturated brine, and the solvent was evaporated. The obtained residue was dissolved in N,N-dimethylformamide (5 mL), 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) (0.12 mL) was added, and the mixture was stirred at room temperature overnight. Water was added to the reaction mixture, and the mixture was extracted with ethyl acetate, the extract was washed with saturated brine, and the solvent was evaporated. The obtained residue was purified by column chromatography (hexane:ethyl acetate) to give the title compound (57 mg).

Provenance & Evidence