Betahistine → 3,5-Dimethyl-2-[4-[4-[2-[N-[2-(2-pyridyl)ethyl]-N-methylamino]ethoxy]benzoyl]benzylthio]-4(3H)-quinazolinone dihydrochloride

Participants

Reaction Steps

A solution of 2-[4-[4-(2-chloroethoxy)benzoyl]-benzylthio]-3,5-dimethyl-4(3H)-quinazolinone (381 mg), 2-(2-methylaminoethyl)pyridine (0.17 ml) and triethylamine (0.33 ml) in DMF (7 ml) was stirred at 100° C. for 21 hours. This reaction mixture was concentrated and the residue was purified by silica gel column chromatography (dichloromethane: methanol: aqueous ammonia =9:1:0.1) and treated with hydrogen chloride/ethyl acetate to provide the title compound as colorless solid (256 mg).

Provenance & Evidence