WE CLAIM:
1. A process for the direct preparation of malic acid salt of sunitinib, wherein the
process comprises:
a) reacting A^-[2-(diethylamino)ethyl]-5-formyl-2,4-dimethyl-l//-pyrrole-3-
carboxamide of Formula II
CH3
N—/
O /
H3C V-NH
OHC-'X^/^-CHa
H
FORMULA II
with 5-fluoro-l,3-dihydro-2i/-indol-2-one of Formula III
H
FORMULA III
in the presence of malic acid and a solvent; and
b) isolating malic acid salt of sunitinib from the reaction mixture thereof
2. A process according to claim 1, wherein the solvent used in step a) is water, an
organic solvent or a mixture thereof
3. A process according to claim 2, wherein the organic solvent is alkanol, ester,
nitrile, aromatic hydrocarbon, cyclic ether, ketone, or a mixture thereof
4. A process according to claim 3, wherein the organic solvent is alkanol.
5. A process according to claim 4, wherein the alkanol is ethanol.
6. A process according to claim 1, wherein step a) is carried out in the presence of a
base.
7. A process according to claim 6, wherein the base is organic amine.
8. A process according to claim 7, wherein the organic amine is pyrrolidine.
9. A process according to claim 1, wherein the malic acid used in step a) is L-malic
acid or D-malic acid, or a mixture thereof.