Benzene → Sunitinib

Participants

Reaction Steps

Accordingly, the present invention provides the crystalline Form-C obtained in non-polar alicyclic hydrocarbon solvent like cyclopentane, cyclohexane or cycloheptane. According to the process of the present invention, 5-Formyl-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)-amide (IX) and 5-Fluoro-1,3-dihydro-indol-2-one (X) in aromatic hydrocarbon solvents like benzene or toluene are reacted in presence of catalytic amount of pyrrolidine as base at 80-85° C. for 3-9 hours. The resultant Sunitinib base is again triturated with the same solvent at 80-85° C. for 1-2 hours and isolated at a temperature ranging from 20-45° C., preferably at 25-35° and most preferably at 25-30° C. and dried at 60° C. for 5-20 hours to get Sunitinib base (I) as orange crystalline solid.

Provenance & Evidence