Pyrrolidine → Sunitinib

Participants

Reaction Steps

5-Formyl-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)-amide (10.0 g 0.037 moles) and 5-Fluoro-1,3-dihydro-indol-2-one (5.41 g; 0.0358 moles) in methanol were reacted in presence of catalytic amount of pyrrolidine (0.16 mL) as base at reflux temperature for 2-8 hours. The resultant Sunitinib base was triturated in methanol at reflux temperature 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