Xanthine derivatives

C - Chemistry – Metallurgy – 07 – D

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260/242.4

C07D 473/06 (2006.01)

Patent

CA 1075693

ABSTRACT This invention relates to a process for the preparation of compounds of general formula Image (I) wherein R1 is alkyl having from 2 to 4 carbon atoms, R2 is methyl and R3 is a straight-chained 5-oxohexyl group and physiologically acceptable acid addition salts thereof, which comprises a) reacting an alkali metal salt of an 1,3-dialkylxanthine with a substance selected from the group consisting of i) a compound formula Image (III) wherein A is an alkylene group containing from 3 to 6 carbon atoms and Hal is a halogen atom; ii) a ketal therefrom and in case iii) subsequently hydrolysing the product, or b) reacting an alkali metal salt of a 3-methyl-7-oxohexylxanthine with an alkylating compound selected from the group consisting of alkyl halides and a dialkyl sulphate in the presence of a solvent, or c) reacting a compound of the formula Image (IV) wherein X is an alkylene group containing from 2 to 5 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 in which there are at least 3 carbon atoms between the carbonyl group and the nearest nitrogen atom, or d) oxidation of a compound of the formula Image (V) wherein R1 and R2 are as defined above and Y is a straight-chained 5-hydroxy- hexyl group; and wherein the product formed 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.

320438

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