Hydrogen Bromide → Tofacitinib hydrobromide

Participants

Reaction Steps

An aqueous solution (48 wt %) of hydrogen bromide (3.44 g, 20.4 mmol) was added to a solution of tofacitinib free base (5.60 g, 17.9 mmol) in acetone (30 mL). The resulting oily suspension was stirred for 1 hour at 25° C. before acetone was removed in vacuo by rotary evaporation and the residual solid was dried under vacuum (8 torr) for 16 hours at 25° C. to yield 7.08 g of amorphous tofacitinib hydrobromide as a pale orange solid. 1H NMR analysis showed a residual acetone content of approximately 1.0 wt %.

Provenance & Evidence