Sodium Bicarbonate → (+)-Sibutramine

Participants

Reaction Steps

The filtrate obtained by filtration after reacting with L-DBTA was neutralized to pH 8.5 with sodium hydroxide, and then extracted with chloroform to obtain (+)-sibutramine, which was nearly pure (+)-isomer. D-DBTA was added thereto to obtain crystals and the crystals were recrystallized from 450 ml of isopropyl alcohol to obtain D-DBTA salt of (+)-sibutramine (ee: ≧99.3%). The D-DBTA salt of (−)-sibutramine was neutralized to pH 8.5 with saturated sodium bicarbonate, and then extracted with chloroform to obtain (+)-sibutramine free base.

Provenance & Evidence