Alkanophenones

Details Alkanophenones Alkanophenones

C - Chemistry, Metallurgy

07

D

167/233, 167/244

C07D 311/24 (2006.01) A61K 31/35 (2006.01) C07D 405/04 (2006.01)

Patent

CA 1340463

-1- Substituted alkanophenones of general formula Image in which R1 is unsubstituted or fluorinated lower alkyl, R2 is hydrogen, or unsubstituted or fluorinated lower alkyl or lower alkenyl, X is lower alkylene, oxy, thio or a direct bond, alk is lower alkylene, n is 1 or 2, R3 is phenyl that is unsubstituted or is substituted by unsubstituted or fluorinated lower alkyl, by etherified or esterified hydroxy, by unsubstituted or lower alkylated amino and/or by free, esterified or amidated carboxy, or is lower alkyl that is unsubstituted or fluorinated or substituted by free, esterified or amidated carboxy, R4 is free, esterified or amidated carboxy or 5-tetrazolyl, and R5 is hydrogen or lower alkyl, have leucotriene-antagonistic properties and can be used as anti-allergic active ingredients in medicaments. The process for their preparation comprises reacting an epoxide of formula Image in which R1, R2, X, alk, n and R3 are as defined above, with a thiol of formula -2- Image in which R4 and R5 are as defined above, or with a salt thereof, and, if desired, converting a compound obtainable in accordance with the process into a different compound of formula I, separating a stereo-isomeric mixture obtainable in accordance with the process into the components and/or converting a free compound obtainable in accordance with the process into a salt, or converting a salt obtainable in accordance with the process into the free compound or into a different salt.

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