XANTHINE DERIVATIVES

• Main Authors: KOMAREK, JAROMIR, JAYME, MANFRED, MOHLER, WERNER
• Format: Patent
• Language: English; French
• Published: 15.04.1980
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY

This invention relates to a process for the preparation of the compounds of general formula (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 comprisesa) 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 (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, orb) 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, orc) reacting a compound of formula (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, ord) oxidation of a compound of formula (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.