TICAGRELOR synthesis

Yield:-

Reaction Conditions:

in water at 20; for 24 h;

Steps:

13

Example 13; Synthesis of N-methyl-4-(4-ureidophenoxy)picolinamide (Compound 6); A solution of sodium cyanate (5.5 g, 0.0846 mol) in water (55 ml) was prepared. This clear solution was then added to the stirred solution of 4-(4-aminophenoxy)-N-methylpicolinamide hydrochloride (V) (25 g, 0.0894 mol) in water (125 ml) drop wise maintaining ambient temperature of the reaction mass. The reaction mass was then stirred for 24 hours at the same temperature and the obtained solid was then filtered, washed thoroughly with water and vacuum dried at 80° C. to obtain (16 g) of the N-methyl-4-(4-ureidophenoxy)picolinamide.

References:

US2010/311980,2010,A1 Location in patent:Page/Page column 22