Amine acid salt compounds and process for the production thereof
OwnerSeo Hong Yooinventor
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Abstract
A stoichiometric acid moiety transfer reaction for the preparation of an acid salt of an amine compound is disclosed. The acid moiety transfer reaction provides amine acid salts of high purity and having crystalline structure of uniform size and shape.
Claims46
A method for preparing an acid salt of an amine compound which comprises placing a donor compound having at least one amine acid salt moiety in solution with a free amine compound, said donor compound having a pka below at least the highest pka of the free amine compound, to provide a transfer of acid salt moiety from the donor compound to the free amine compound, yielding as the product thereof an amine acid salt of the free amine compound.
A method for preparing an acid salt of an amine compound which comprises placing an approximately equimolar amount of dimethylpyridine hydrochloride in solution with a free amine compound, said dimethylpyridine hydrochloride having a pKa below at least the highest pKa of the free amine compound, to provide a transfer of acid salt moiety from the dimethylpyridine hydrochloride to the free amine compound, yielding as the product thereof a monoacid salt of ranitidine hydrochloride.
A method for preparing Form I ranitidine n hydrochoride which is substantially free of Form II ranitidine hydrochloride comprising
- treating ranitidine free base with a donor compound capable of transferring HCl to the ranitidine free base in a solvent solution having a polarity suitable for precipitating the Form I ranitidine hydrochloride.
A method for preparing form I ranitidine n hydrochloride which is substantially free of form II ranitidine n hydrochloride comprising
- treating ranitidine free base with a donor compound selected from the group consisting of pyridine HCl, dimethylpyridine HCl, chloropyridine HCl, quinoline HCl and derivatives thereof.
A method for removing impurities from a mixture of an amine acid salt compound comprising more than one species of said amine acid salt compound comprising
- placing said mixture in solution with a free amine compound having a pKa value between two pKa values of the mixture of amine acid salt compound, to provide a selective transfer of acid salt moiety from the amine acid salt compounds comprising said mixture to the free amine to thereby remove impurities, yielding as the product thereof a single species of amine acid salt compound.
A method for removing impurities from a mixture of an amine acid salt compound comprising more than one species of ranitidine hydrochloride comprising
- placing said mixture in solution with pyridine having a pKa value between the two pKa values of the amino acid salt, to provide a selective transfer of acid moiety from the rantidine hydrochloride species to the pyridine to thereby remove impurities, yielding as a product thereof a single species of ranitidine hydrochloride.
Dependencies are inferred from the claim text.