Pure erlotinib
AssigneeGenerics [UK] Limited
InventorsVinayak Govind Gore, Anilkumar Tripathi, Madhav Jadhav
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Abstract
The present invention relates to processes for the preparation of erlotinib and salts and polymorphs thereof, preferably of high purity. The present invention also relates to erlotinib and salts and polymorphs thereof preparable by said processes, to medical uses of said erlotinib, salts and polymorphs, and to pharmaceutical compositions comprising the same.
Claims31
1-62. (canceled)
A process for the preparation of erlotinib base, or a salt thereof, comprising reacting 4-chloro-6,7-bis-(2-methoxyethoxy)quinazoline and 3-ethynylaniline in a reaction solvent, wherein the reaction mixture does not contain an external acid or base.
A process for the preparation of erlotinib base, comprising reacting a salt of erlotinib with a base in a solvent consisting of:
- (a) methanol and/or ethanol;
- and
- (b) optionally water.
A process for the preparation of erlotinib base, comprising reacting a salt of erlotinib with a carbonate or bicarbonate base in a solvent consisting of one or more polar protic solvents.
A process for the preparation of erlotinib base, comprising the crystallisation of erlotinib base from a solvent comprising a straight chain, branched or cyclic C4 to C20 alcohol.
Erlotinib base or a salt thereof with a HPLC purity of:
- (a) more than 99.0%;
- or
- (b) more than 99.5%;
- or
- (c) more than 99.8%;
- or
- (d) more than 99.9%.
A process for the preparation of erlotinib hydrochloride form A, comprising crystallization of erlotinib hydrochloride from a solvent.
A process for the preparation of erlotinib hydrochloride form A, comprising dissolving erlotinib base in a solvent, mixing with aqueous or non-aqueous HCl and crystallization of erlotinib hydrochloride from the solvent.
Erlotinib hydrochloride form A, comprising less than 3% (w/w) of erlotinib hydrochloride in form B or other polymorphic forms.
Dependencies are inferred from the claim text.