Process for 1h-imidazo[4,5-c]quinolines

C - Chemistry – Metallurgy – 07 – D

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260/246.1, 260/2

C07D 215/42 (2006.01) C07D 471/04 (2006.01)

Patent

CA 2027245

Disclosed is a process for the preparation of 1-substituted, 4-substituted-1H-imidazo[4,5-c]quinolines of the formula: Image wherein R1 is alkyl, alkenyl, and substituted alkenyl wherein the substituent is alkyl, cycloalkyl and cycloalkyl substituted by lower alkyl; substituted alkyl, wherein the substituent is lower alkyl, cycloalkyl and cycloalkyl substituted by lower alkyl; hydroxyalkyl and dihydroxy-alkyl; R2 is hydrogen; alkyl, benzyl, (phenyl)ethyl and phenyl, the benzyl, (phenyl)ethyl or phenyl substituent being optionally substituted on the benzene ring by one or two moieties independently selected from the group consisting of lower alkyl, lower alkoxy and halogen, with the proviso that when the benzene ring is substituted by two such moieties, then the moieties together contain no more than 6 carbon atoms; each R is lower alkoxy, halogen, or lower alkyl, and n is an integer from zero to 2, with the proviso that if n is 2, then the R groups together contain no more than 6 carbon atoms. Also disclosed are intermediates for use in the preparation of such compounds which are useful as bronchodilators or antiviral agents depending on the nature of substituent R4, and processes for the preparation of such intermediates.

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