Pyrrolidine → Sunitinib

Participants

Reaction Steps

5-Formyl-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)-amide (5.0 g 0.018 moles) and 5-Fluoro-1,3-dihydro-indol-2-one (2.705 g; 0.018 moles) in toluene were reacted in presence of catalytic amount of pyrrolidine (0.08 mL) as base at 80-85° for 2-8 hours. The resultant Sunitinib base was triturated in toluene at 80-85° for 1-2 hours and isolated at 25-30° C. and dried at 60° C. for 5-20 hours to get Sunitinib base (I) as orange crystalline solid.

Provenance & Evidence