ALKANOPHENONES

• Main Authors: VON SPRECHER, ANDREAS, BECK, ANDREAS
• Format: Patent
• Language: English; French
• Published: 23.03.1999
• Edition: 6
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

Substituted alkanophenones of general formula 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 in which R1, R2, X, alk, n and R3 are as defined above, with a thiol of formula 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.