Selective n-sulfonylation of 2-amino trifluoroalkyl...

C - Chemistry – Metallurgy – 07 – D

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C07D 333/34 (2006.01) C07C 303/38 (2006.01) C07C 311/17 (2006.01)

Patent

CA 2637615

Processes for the preparation of trifluoroalkyl substituted N-(2-hydroxyalkyl) heteroarene- and benzenesulphonamide derivatives of formula (I) or formula (II) (wherein the variables are as defined in the claims) are provided which comprises reacting a trifluoroalkyl substituted amino alcohol, a sulphonyl chloride and a base/solvent system selected from the group consisting of (a) 4- methylmorpholine/isopropyl acetate, (b) Hünig's base/tetrahydrofuran, (c) 4- methylmorpholine/acetonitrile, (d) 4-methylmorpholine/propionitrile and (e) 4- methylmorpholin/ftoluene. Formulae (I) and (II).

La présente invention concerne des procédés de préparation de dérivés de N-(2-hydroxyalkyl) hétéroarène-sulfamide et benzène-sulfamide porteurs d'une substitution par un trifluoroalkyle de formule I ou de formule II (dont les variables sont telles que définies dans les revendications). Lesdits procédés comprennent la réaction d'un alcool aminé porteur d'une substitution par un trifluoroalkyle, d'un chlorure de sulfonyle et d'un système base/solvant choisi dans le groupe qui comprend (a) un acétate de 4-méthylmorpholine/isopropyle, (b) une base de Hünig/tétrahydrofuranne, (c) un 4-méthylmorpholine/acétonitrile, (d) un 4-méthylmorpholine/propionitrile et (e) un 4-méthylmorpholine/toluène.

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