Xanthine derivatives

C - Chemistry – Metallurgy – 07 – D

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260/242.4

C07D 473/06 (2006.01)

Patent

CA 1075691

ABSTRACT This invention relates to a process for the preparation of the compounds of general formula Image (I) wherein R1 is a straight-chain 5-oxohexyl group, R2 is alkyl having at most 2 carbon atoms and R3 is a straight-chain or branched alkyl group containing from 2 to 4 carbon atoms, and physiologically acceptable acid addition salts thereof, which comprises a) reacting an alkali metal salt of a 3-methyl- or 3-ethyl-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 4 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-(5-oxohexyl)-3-methyl- or 3-ethyl-xanthine with an alkylating compound selected from the group consisting of alkyl halides and a dialkyl sulphate wherein the alkyl group or groups contain 2 to 4 carbon atoms in the presence of a solvent, or c) reacting a compound of formula Image (IV) wherein X is an alkylene group containing 3 carbon atoms and Hal is a halogen atom with an alkali metal salt of an acetoacetate and subsequently 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 a 5-hydroxyhexyl group; and wherei.n the product obtained is isolated per se or reacted with an acid to form a physiologically compatible 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.

320436

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