| 摘要 |
4-17747/+ Further novel alkanophenones Substituted alkanophenones of the general formula (I), 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 a 5-membered heteroaryl radical that contains 1 N, O or S atom as hetero atom and 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, 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 antiallergic active ingredients in medicaments. The process for their preparation comprises reacting an epoxide of formula II (II), in which R1, R2, X, alk, n and R3 are as defined above, with a thiol of formula III (III), in which R4 and R5 are as devined 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 stereoisomeric mixture obtainable in accordance with the process into its components and/or converting a free compound obtainable in accordance with the process into a salt, or a salt obtainable in accordance with the process into the free compound or into a different salt.
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