Hydrochloric Acid → HCID 178434483, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of 8.5 g of pyridine and 10 mL of concentrated hydrochloric acid was heated to 230° C., added to EXAMPLE 1 (217 mg, 1.0 mmol) and the mixture heated at 230° C. for 2 hours. After cooling, water was added and the suspension neutralized with 10% sodium hydroxide. Dichloromethane (50 mL) was added, the mixture was filtered and the solid collected, washed with dichloromethane and water and dried. Purification by HPLC (Zorbax, C-18, 250×2.54 column, Mobile phase A: 0.1% trifluoroacetic acid in water; B: 0.1% trifluoroacetic acid in acetonitrile; 0-100% gradient) provided 173 mg (73%) of the title compound as the trifluoroacetate salt. 1H NMR (DMSO-d6) 1.63-1.73 (m, 4H), 2.29-2.34 (m, 2H), 2.46 (s, 3H), 2.75-2.80 (m, 2H), 11.28 (br s, 1H).

Provenance & Evidence