反应详情

4-(4-(3-(4-chloro-3-(trifluoromethyl)phenyl)ureido)phenoxy)-N-methylpicolinamide (sorafenib base) (100 g, 0.2152 mol) was suspended in acetone (1000 ml) at ambient temperature. p-toluene sulfonic acid (50 g, 0.290 mol) was dissolved in acetone (500 ml) and this solution was charged to above reaction mass drop wise in 15 minutes. The obtained precipitate was stirred for 1-2 hours at ambient temperature, filtered and washed with acetone (500 ml). It was vacuum dried for 12 hours at 50° C. to afford 4-(4-(3-(4-chloro-3-(trifluoromethyl)phenyl)ureido)phenoxy)-N-methylpicolinamide tosylate (Sorafenib Tosylate) (130 g).

1. additionthis solution was charged to above reaction mass drop wise in 15 minutes
2. filtrationfiltered
3. washwashed with acetone (500 ml)
4. customdried for 12 hours at 50° C.