Substituted acetophenones and process therefor

C - Chemistry – Metallurgy – 07 – C

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C07C 49/82 (2006.01) C07C 45/74 (2006.01) C07C 49/84 (2006.01) C07C 69/02 (2006.01) C07D 207/333 (2006.01) C07D 213/50 (2006.01) C07D 213/80 (2006.01) C07D 241/24 (2006.01) C07D 307/40 (2006.01) C07D 307/46 (2006.01) C07D 317/54 (2006.01) C07D 333/22 (2006.01)

Patent

CA 1124254

ABSTRACT Process for the preparation of antivirally active compounds of the formula Image II wherein R1' represents hydroxy, acyloxy derived from an aliphatic acid having 2-18 carbon atoms or a heterocyclic carboxylic acid containing mitrogen atom(s), lower alkoxycarbonyloxy, aminoacyloxy or carboxyalkanoyloxy; R2' represents lower alkoxy; R3' represents lower alkoxy; and R4' represents phenyl which is substituted by one or more substituents selected from the group consisting of lower alkyl, lower alkoxy, benzyloxy, allyloxy, alkylthio, dealkylamino, amino and cyano; lower slkyl-substi- tuted furyl or pyridyl, thienyl or pyrrolyl which may be substituted by lower alkyl, with the provise that when R4' is p-methoxyphenyl, R1' is a radical other than acetoxy, which process comprises a) reacting a compound of the formula Image III wherein R2' and R3' are as defined above, with an aldehyde or formula R4'-CH0 IV wherein R4' is as defined above, in an organic solvent in the presence of a basic cata- lyst, or b) reacting a compound of formula Image V wherein R2', R3' and R4' are as defined above, and M represents a hydrogen atom or an alkali metal, with an acid anhydride or an acid halide derived from an aliphatic mono- or dicarboxylic acid having 2-18 car- bon atoms, a heterocyclic carboxylic acid containing ni- trogen atom(s) or an amino acid in an organic solvent and pharmaceutical compositions containing them.

343964

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