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    • 6. 发明申请
    • Process for The Preparation of Sulfonic Acid Salts of Oxabispidines
    • 制备Oxabispidines磺酸盐的方法
    • US20080200673A1
    • 2008-08-21
    • US11993026
    • 2006-06-12
    • Lal CheemaDavid Cladingboel
    • Lal CheemaDavid Cladingboel
    • C07D498/08
    • C07D498/08
    • There is provided a process for the isolation of a sulfonic acid salt of formula I, or a solvate thereof, from a mixture comprising: (i) the corresponding free base; and (ii) a compound of formula III. or a salt and/or solvate thereof, which process comprises providing an aqueous dispersion of the compounds of formulae II and III and a source of R3SO3− anions and then, if necessary, adjusting the pH of the aqueous dispersion to any value from 3 to 8. There are further provided processes wherein the mixture of compounds of formulae II and III is provided by incomplete reaction, for example in the presence of base and an aqueous phase, between a compound of formula III and a compound of formula IV In such processes, the RSO3− anions of the resulting salt of formula I may be derived from the compound of formula IV. Also for all of these processes, D, R1, R2 and R3 have meanings given in the description.
    • 提供了从包含以下物质的混合物中分离式I的磺酸盐或其溶剂合物的方法:(i)相应的游离碱; 和(ii)式III化合物。 或其盐和/或溶剂化物,该方法包括提供式II和III化合物的水分散体和R 3 SO 3 SO 3的源, 阴离子,然后如果需要,将水分散体的pH调节至3至8的任何值。还提供了其中提供式II和III化合物的混合物的方法 通过不完全反应,例如在碱和水相存在下,在式III化合物与式IV化合物之间。在这些方法中,RSO 3 - 得到的式I的盐的阴离子可以衍生自式IV化合物。 同样对于所有这些方法,D,R 1,R 2和R 3都具有说明书中给出的含义。