Xanthine derivatives

C - Chemistry – Metallurgy – 07 – D

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260/242.4

C07D 473/06 (2006.01)

Patent

CA 1075692

A B S T R A C T This invention relates to a process for the preparation of the compounds of general formula Image (I) wherein R1 is an (.omega.-1)-oxoalkyl group containing from 5 to 7 carbon atoms, R2 is methyl and R3 is propyl, and physiologically acceptable acid addition salts thereof, which comprises a) reacting an alkali metal salt of a 3-methyl-7-alkyl xanthine with a substance selected from the group consisting of a 1) a compound of formula Image (III) wherein A is an alkylene group containing from 3 to 5 carbon atoms and Hal is a halogen atom; b 1) an acetal, c 1) ketal and d 1) thioketal therefrom and subsequently hydrolysing the product or b) reacting an alkali metal salt of 1-(.omega.-1)-oxoalkyl-3-methyl- xanthine wherein the oxoalkyl radical has from 5 to 7 carbon atoms with a propylating compound selected from the group consisting of propyl halides and a propyl sulphate in the presence of a solvent, c) reacting a compound of formula (IV) Image herein X is an alkylene group containing from 3 to 5 carbon atoms and Hal is a halogen atom with an alkali metal salt of an acetoacetate and subse- quently subjecting the reaction product to ketone splitting to obtain a product of general formula (I) as defined above, or d) oxidation of a compound of formula Image (V) wherein R2 and R3 have the meaning as defined above and Y is an (.omega.-1)-hydroxy- alkyl group having from 5 to 7 carbon atoms, and wherein the product obtained is isolated per se or reacted with an acid to form a physiologically compat- ible acid addition salt thereof. It also relates to the products of this process which are useful in the treatment of diseases involving deficiencies in the blood vascular system.

320437

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