Preparation of lamivudine form I

A thermodynamically controlled process for preparing Form I polymorph of lamivudine is described, wherein the process involves crystallizing Form I at a temperature of from about 0° C. to about 50° C. from a mixture which comprises (a) lamivudine or an acid salt thereof or both, (b) a solvent system...

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Bibliographic Details
Main Authors COTE AARON S, WAHL CHRISTOPHER, ARROYO ITZIA Z, COHEN BENJAMIN
Format Patent
LanguageEnglish
Published 05.08.2014
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Summary:A thermodynamically controlled process for preparing Form I polymorph of lamivudine is described, wherein the process involves crystallizing Form I at a temperature of from about 0° C. to about 50° C. from a mixture which comprises (a) lamivudine or an acid salt thereof or both, (b) a solvent system comprising water and at least one organic solvent, and optionally (c) Form I seed; wherein, when a lamivudine acid salt is employed in the mixture, the crystallizing step is conducted in the presence of a base; and wherein the water activity of the solvent system is maintained in a range in which Form I is thermodynamically the most stable form of lamivudine.
Bibliography:Application Number: US201113577584