1,4-Dioxane → 2-{4-[(3,4-Dichlorophenyl)sulfonyl]piperidin-1-yl}-3-(trifluoromethyl)pyridine

Participants

Reaction Conditions

Reaction Steps

A mixture of the amine from Step 7D (200 mg, 0.68 mmol), 2-chloro-3-(trifluoromethyl)pyridine (200 mg, 1.36 mmol), DIEA (0.36 mL, 2.04 mmol), and 1,4-dioxane (0.10 mL) was heated in the Emrys Creator microwave to 200° C. for 1 h. The mixture was diluted with sat. NH4Cl (20 mL) and EtOAc (50 mL). The organic phase washed with 10% HCl (25 mL), H2O (3×25 mL), and brine (25 mL), dried (MgSO4), and concentrated. The resulting yellow oil was purified by SiO2 chromatography (elution with 10 to 30% EtOAc-hexanes), and lyophilized to afford the title compound (0.19 g), a white solid, 64%.

Provenance & Evidence