| 摘要 |
Preparation of heterocyclyl di- or trifluorobutenyl sulfones or sulfoxides (I) involves reaction of a corresponding thioether (II) with a salt (III) of peroxo-monosulfuric acid. Preparation of sulfones or sulfoxides of formula Het-S(O) n-CH 2CH 2-C(R 1>)=CF 2 (I) involves reaction of a corresponding thioether of formula Het-S-CH 2CH 2-C(R 1>)=CF 2 (II) with a salt (III) of peroxo-monosulfuric acid (H 2SO 5), optionally in presence of a reaction auxiliary and/or diluent. n : 1 or 2; R 1>H or F; Het : 4-(R 2>)-3-(R 3>)-thiazol-2-yl, 4-(R 2>)-3-(R 3>)-oxazol-2-yl, 4-(R 2>)-3-(R 3>)-imidazol-2-yl, 5-(R 3>)-1,3,4-oxadiazol-2-yl, 5-(R 3>)-1,3,4-thiadiazol-2-yl, 6-(R 2>)-4,5-dihydro-6H-1,3-thiazin-2-yl, 1,2,3-thiadiazol-5-yl, pyridin-2-yl, pyrimidin-2-yl, pyridazin-3-yl, benzothiazol-2-yl, benzoxazol-2-yl, 1-(R 4>)-1H-tetrazol-5-yl or a dithiaza-heterocyclic group of formula (a); R 2>H, halo, alkyl or haloalkyl; R 3>H or halo; or alkyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkoxycarbonyl, alkoxyalkyl, alkylthioalkyl, COOH, alkylaminocarbonyl, 3-6C cycloalkylaminocarbonyl, dialkylaminocarbonyl, alkenyl, alkenylthio, alkenylsulfinyl or alkenylsulfonyl (all optionally substituted by halo, alkyl or alkoxy); R 4>1-8C alkyl, 2-6C alkenyl, haloalkyl, alkoxyalkyl, alkylthioalkyl or 3-8C cycloalkyl; or phenyl or benzyl (both optionally substituted by halo, alkyl, alkoxy, alkylthio or haloalkyl); p : 1-3; Y : methylene (optionally mono- or disubstituted, e.g. by alkyl, alkenyl or alkynyl (all optionally substituted by halo, alkoxy, alkylthio, haloalkoxy or haloalkylthio) or phenyl (optionally mono-, di- or trisubstituted, e.g. by halo, CN, NO 2, alkyl, alkoxy, alkylthio, haloalkyl, haloalkoxy or haloalkylthio)); alkyl moieties have 1-4C and alkenyl or alkynyl moieties 2-4C unless specified otherwise. [Image] An independent claim is included for the preparation of the sulfones (I; n =2) by reaction of the sulfoxides (I; n = 1) with (III), optionally in presence of a reaction auxiliary and/or diluent. |
