- PROCESS FOR PREPARING (4S, 6S)-4-(ETHYLAMINO)-5,6-DIHYDRO-6-METHYL-4H-THIENO-[2,3-B]THIOPYRAN-2-SULFONAMIDE-7,7-DIOXIDE AND ITS INTERMEDIATES
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Disclosed herein is an improved process for the preparation of (4S,6S)-4-(ethylamino)-5,6-dihydro-6-methyl-4H-thieno-[2,3-b]thiopyran-2-sulfonamide-7,7- dioxide (Dorzolamide) and its intermediates.
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Page/Page column 14-15
(2011/09/19)
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- PROCESS FOR PREPARING DORZOLAM IDE
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There is provided a process for preparing dorzolamide and processes for preparing intermediates useful in the preparation of dorzolamide. In particular, there is provided a process for preparing an acetoamido sulfone of formula (viii) comprising oxidation of a hydroxysulfonamide of formula (vii) in the presence of an oxidizing agent selected from the group consisting of: a peracid, tert-butyl hydroperoxide, dimethyl dioxirane, selenium dioxide, m-phenanthroline di-N-oxide, nitric acid and hydrogen peroxide. There is also provided a process for preparing an acetoamidosulfone of formula (ix-a) comprising converting a hydroxysulfone of formula (viii) to the acetoamidosulfone of formula (ix-a) in the presence of acetonitrile and an acid. There is also provided a process for separating the cis- and trans-isomers of dorzolamide from a mixture of the trans-isomer of dorzolamide and the cis-isomer of dorzolamide comprising reacting the mixture of isomers with a carboxylic acid.
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Page/Page column 21
(2009/01/20)
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- PROCESS FOR PREPARING DORZOLAMIDE
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A process for resolving dorzolamide trans racemate, which comprises reacting said racemate with (1S) - (+) -10-camphorsulfonic acid so obtaining the (4S, 6S) enantiomer by selectively precipitating and recovering the camphorsulfonic acid salt thereof (dor
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Page/Page column 6-7
(2008/06/13)
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