- Asymmetric syntheses of (S)-Fenfluramine using Sharpless Epoxidation Methods
-
We describe one synthesis of (S)-fenfluramine and several syntheses of its precursors (R)- and (S)-1-(meta-trifluoromethylphenyl)propan-2-ols.They were obtained from the asymmetric epoxidation of the primary allylic alcohol 5 and from the kinetic resolution with asymmetric epoxidation of teh secondary allylic alcohol 6.
- Goument, Bertrand,Duhamel, Lucette,Mauge, Robert
-
p. 171 - 188
(2007/10/02)
-
- Alkanophenones useful for treating allergies
-
Substituted alkanophenones of general formula STR1 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, substituted by fluoro and chloro 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.
- -
-
-
- Aromatic thioethers
-
Novel asymmetric thioethers of the formula STR1 in which the general symbols have the following meanings: R0 represents hydrogen or C1-7 -alkanoyl, R1 represents C1-3 -alkyl which may be substituted by one or more halogen atoms having an atomic number of at most 17, R2 represents an aliphatic radical having from 5 to 15 carbon atoms, A represents ethylene, a single bond or vinylene, B1 represents C1-7 -alkylene or phenylene, B2 represents a single bond, ethylene or phenylene, and M represents an aromatic radical of the partial formula STR2 in which the symbols have the following meanings: R3 represents hydrogen or C1-4 -alkyl, X represents NH, O, S or if R4 represents hydrogen, a single bond, one of the symbols R4 and R5 represents hydrogen and the other represents the group --CO--R6, or R4 and R5 together represent the radical --CO--C(R6)=C(R7)--or--CO--C(R7)=C(R6)--or R4 R5, together with X, represent the radical --N=C(R8)--C(R6)=CH--, in which R6 represents --(CH2)b --COOR3 (in which b=0 to 2) R7 represents hydrogen or C1-4 -alkyl and R8 represents hydrogen, methyl, mythoxy or halogen, and their salts are active as leucotriene antagonists since they eliminate the contractions of smooth muscles brought about by leucotrienes, and are therefore suitable for the treatment of allergic, especially asthmatic, conditions.
- -
-
-