Sertraline → Sertraline Hydrochloride

Participants

Reaction Steps

Sertraline base (27 kg) was dissolved in 105 kg of n-butanol. The solution was treated for 1 hour with 1 kg carbon at 40 to 45° C. and filtered and washed with 25 kg n-butanol. The solution was reheated to 40-45° C. and the achieved temperature was kept constant during the gas flow and filtration. Hydrogen chloride gas was added at the rate of 4.5-5 kg/hr for the duration of 1 hour until pH 0.5 or less was reached. Immediately thereafter, the slurry was filtered at 40-45° C. The cake was washed with 25 kg of n-butanol, and dried for about 4 hours at 80° C. The yield was 70% (21.2 kg).

Provenance & Evidence