1) A process for the preparation of Selumetinib intermediate of Formula (VI),
comprising the steps of:
Formula (VI)
(a) reacting a compound of Formula (II) with a compound of Formula (III) to give a
compound of Formula (IV);
Formula (II) Formula (III) Formula (IV)
(b) reducing a compound of Formula (IV) to produce a compound of Formula (V).
(c) cyclization of compound of Formula (V) to produce a compound of Formula (VI).
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2) The process according to claim 1, the reducing agent is selected from sodium
dithionite, sulfur, sodium sulfide, sodium hydrogen sulfide, palladium on carbon,
platinum on carbon, Raney Ni, Pd-BaSO4, Pd-CaCO3, Fe, Zn, SnCl2, B2pin2, B2(OH)4
NaBH4, formic acid.
3) The process according to claim 1, the solvent is selected from toluene, xylene,
chlorobenzene, tetralin, methanol, ethanol, isopropyl alcohol, n-butanol, 1-propanol,
acetone, ethyl methyl ketone, diethyl ketone, methyl isobutyl ketone, C3-C6 ketones,
dichloromethane, chloroform, n-pentane, n-hexane, n-heptane, diethyl ether,
diisopropyl ether, tert-butyl methyl ether, dibutyl ether, tetrahydrofuran, 1,2-
dimethoxyethane, 2-methoxyethanol, 2-ethoxyethanol, anisole, 1,4-dioxane,
acetonitrile, propionitrile, C2-C6 nitriles, ethyl formate, methyl acetate, ethyl acetate,
propyl acetate, butyl acetate, methyl propanoate, ethyl propanoate, methyl butanoate,
ethyl butanoate, dimethyl formamide, dimethylacetamide, Nmethylpyrrolidine (NMP),
formamide, acetamide, propanamide, dimethyl sulfoxide and water.
4) A process for the preparation of Selumetinib comprising converting Selumetinib
intermediate of Formula (VI), as prepared by a process of the present application to
Selumetinib.
Dated 28
th day of December 2022 ____________________
Dr. B. Dinesh Kumar
Dr. Reddy’s Laboratories Ltd
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TITLE OF THE INVENTION: “PROCESS FOR THE PREPARATION OF
SELUMETINIB AND ITS INTERMEDIATES”