Process for the preparation of anastrozole and intermediates thereof
AssigneeGlenmark Pharmaceuticals S.A.
InventorsAnil Khile, Narendra Joshi, Shekhar Bhirud
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Abstract
A process for the preparation of anastrozole is provided, the process comprising: (a) reacting 3,5-bis(1-cyano-1-methylethyl)benzyl halide with a 4-Z-1,2,4-triazole compound of the formula wherein Z is a protecting group to produce 2,2′-[5-(4-Z-1,2,4-triazolium-1-ylmethyl)-1,3-phenylene]di(2-methylpropionitrile) halide; and (b) deprotecting the 2,2′-[5-(4-Z-1,2,4-triazolium-1-ylmethyl)-1,3-phenylene]di(2-methylpropionitrile)halide to produce anastrozole. Also provided is anastrozole substantially free of its isomers.
Claims34
A process for the preparation of a compound of Formula III:
- wherein X is a halide and Z is a protecting group, the process comprising reacting a 3,5-bis(1-cyano -1-methylethyl)benzyl halide with a 4-Z-1 ,2,4-triazole compound of the formula
- wherein Z has the aforementioned meaning.
A compound of Formula III:
- wherein X is a halide and Z is a protecting group.
A process for the preparation of anastrozole comprising:
- (a) reacting a 3,5-bis(1-cyano-1-methylethyl)benzyl halide with a 4-Z-1,2,4-triazole compound of the formula
- wherein Z is a protecting group to produce a compound of Formula III:
- wherein X is a halide and Z has the aforementioned meaning;
- and
- (b) deprotecting the compound of Formula III to produce anastrozole.
Substantially pure anastrozole.
Dependencies are inferred from the claim text.