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    • 96. 发明申请
    • PROCESS FOR PREPARING DORZOLAM IDE
    • 制备DORZOLAM IDE的方法
    • WO2008135770A2
    • 2008-11-13
    • PCT/GB2008/001592
    • 2008-05-07
    • CIPLA LIMITEDCURTIS, Philip, AnthonyKANKAN, Rajendra, NarayanraoRAO, Dhanmaraj, RamachandraMUDGAL, Shrikant, Suresh
    • KANKAN, Rajendra, NarayanraoRAO, Dhanmaraj, RamachandraMUDGAL, Shrikant, Suresh
    • C07D495/04
    • C07D495/04
    • 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.
    • 提供了制备多佐胺的方法和制备可用于制备多佐胺的中间体的方法。 特别地,提供了制备式(viii)的乙酰胺基砜的方法,包括在选自以下的氧化剂的存在下氧化式(vii)的羟基磺酰胺:过酸,叔丁基过氧化氢, 二氧杂环己烷,二氧化硒,间二菲咯啉二-N-氧化物,硝酸和过氧化氢。 还提供了制备式(ix-a)的乙酰氨基砜的方法,包括在乙腈和酸存在下将式(Ⅸ)的羟基砜转化成式(ix-a)的乙酰胺基砜。 还提供了从多佐胺的反式异构体和多佐胺的顺式异构体的混合物中分离多佐胺的顺式和反式异构体的方法,包括使异构体的混合物与羧酸反应。