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US 2008/0076933 A1Published application
Process for making anastrozole
OwnerMichal Benes, Zdenek Prosek +2inventors
InventorsMichal Benes, Zdenek Prosek, Jiri Hykl, Jaroslav Pis
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Abstract
A process for making anastrozole using a 1-substituted triazole can reduce formation of the undesired iso-anastrozole. A typical process is represented by wherein compound (10) is a 1-substituted triazole and compound (1) is anastrozole.
Claims18
A process, which comprises:
- reacting a 1-substituted 1,2,4-triazole selected from the group consisting of
- a 1-(p-toluenesulfonyl)-1,2,4-triazole of formula (10),
- a sulfenylditriazole of formula (11), and
- a carbonylditriazole of formula (12)
- with a metal salt of 2-[3-(cyano-dimethyl-methyl)-5-hydroxymethyl-phenyl]-2-methyl-propionitrile of formula (5)
- wherein M represents a metal, in a solvent to form anastrozole of formula (1)
3 more elements
A process of making a pharmaceutical grade anastrozole comprising the steps of:
- a) reacting a compound of formula (5a) with a compound of formula (10):
- to provide anastrozole in a reaction mixture;
- b) isolating anastrozole from said reaction mixture as a base or as an acid addition salt to obtain crude anastrozole;
- c) dissolving said crude anastrozole in a mixture of water and a water miscible C1-C4 aliphatic alcohol, optionally in the presence of up to 2 molar equivalents of an acid, and crystallizing to form purified anastrozole;
- and
- d) recrystallizing the purified anastrozole from a mixture of water and water miscible C1-C4 aliphatic alcohol.
3 more elements
A compound of formula (5a)
A compound of formula (1a)
Dependencies are inferred from the claim text.