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US 7,247,744 B2Granted
Process for the preparation of probucol derivatives
AssigneeCambrex Charles City, Inc.
InventorPaul Alan Jass
Life of this patent
Estimating the term…
Abstract
A method is described for the preparation of polymorphic forms of water-soluble derivatives of probucol compounds having the following formula where R1, R2, R3, R4, R5, R6, Z and Z′ are defined herein.
Claims6
A process for the preparation of a water-soluble derivative of probucol having the following formula
- where R1 and R2 are the same or different and are -C1-C6 alkyl, -C3-C6 alkenyl or aryl, R3, R4, R5 and R6 are the same or different and are C1-C6 alkyl, Z and Z′ are the same or different and are hydrogen or the groups that are saturated acyl or unsaturated acyl having from 1 to 8 carbon atoms said saturated acyl or unsaturated acyl containing a polar or charged functionality where Z and Z′ can not both be hydrogen by mixing a probucol compound of the formula
- where R1, R2, R3, R4, R5 and R6 are as previously defined with a carboxylic acid anhydride selected from the group consisting of succinic acid anhydride, glutaric acid anhydride, adipic acid anhydride, suberic acid anhydride, sebacic acid anhydride, azelaic acid anhydride, phthalic acid anhydride or maleic acid anhydride and a prophosphatrane compound of the formula
- where R, R′ and R″ are the same or different and are hydrogen or C1 to C8 alkyl to form a reaction mixture and then separating the water soluble derivative of probucol or the probucol compound from said reaction mixture.
A process for the preparation of a water-soluble derivative of probucol having the following formula
- where R1 and R2 are the same or different and are —C1-C6 alkyl, —C3-C6 alkenyl or aryl, R3, R4, R5 and R6 are the same or different and are C1-C6 alkyl, Z and Z′ are the same or different and are hydrogen or the groups that are saturated acyl or unsaturated acyl having from 1 to 8 carbon atoms said saturated acyl or unsaturated acyl containing a polar or charged functionality where Z and Z′ can not both be hydrogen by mixing a probucol compound of the formula
- where R1, R2, R3, R4, R5 and R6 are as previously defined with a carboxylic acid anhydride selected from the group consisting of succinic acid anhydride, glutaric acid anhydride, adipic acid anhydride, suberic acid anhydride, sebacic acid anhydride, azelaic acid anhydride, phthalic acid anhydride or maleic acid anhydride and a prophosphatrane compound of the formula
- where R, R′ and R″ are the same or different and are hydrogen or C1 to C8 alkyl to form a reaction mixture and then separating the water soluble derivative of probucol or the probucol compound from said reaction mixture.
Dependencies are inferred from the claim text.