Method for obtaining 4-(n-alkylamine)-5,...

C - Chemistry – Metallurgy – 07 – D

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C07D 495/04 (2006.01) C07D 333/00 (2006.01) C07D 335/00 (2006.01)

Patent

CA 2436185

The process for obtaining 4-(N-alkylamino)-5,6-dihydro-4H- thien-(2,3-b)-thiopyran-2-sulfonamide-7,7-dioxides (I) wherein R1 is H or C1-5 alkyl, and R2 is C1-5 alkyl, starts from the corresponding 4-(N-alkylamino)-5,6-dihydro-4H-thien-(2,3-b)-thiopyran-7, 7-dioxides, and comprises protecting the alkylamine group, introducing a sulfonamide group and eliminating protecting group. Some compounds of formula (I) are inhibitors of the carbonic anhydrase and can be used in the treatment of elevated intraocular pressure. (see formula I)

L'invention concerne un procédé d'obtention de 4-(N-alkylamino)-5, 6-dihydro-4H-thieno-(2,3-b)-thiopyran-2-sulfamide-7, 7-dioxydes (I), dans lesquels R1 représente un H ou un alkyle C1-5 et R2 représente un alkyle C1-5, à partir des 4-(N-alkylamino)-5, 6-dihydro-4H-thieno-(2,3-b)-thiopyran-7, 7-dioxydes correspondants, comprenant la protection du groupe alkylamino, l'introduction du groupe sulfamide et la libération du groupe protecteur. Certains composés (I) sont des inhibiteurs de l'anhydrase carbonique et peuvent être utilisés dans le traitement de la pression intra-oculaire élevée.

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