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PROCESS FOR THE PREPARATION OF SULFONIC ACID SALTS OF OXABISPIDINES
PROCESS FOR THE PREPARATION OF SULFONIC ACID SALTS OF OXABISPIDINES
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机译：制备奥沙比西丁的磺酸盐的方法
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摘要
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.
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