Solid state properties and effective resolution procedure for guaifenesin, 3-(2-methoxyphenoxy)-1,2-propanediol |
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| Institution: | 1. Department of Physics, Tomsk State University, 634050 Tomsk, Russia;2. Institute of Physical Chemistry, Bulgarian Academy of Sciences, 1113 Sofia, Bulgaria |
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| Abstract: | Racemic expectorant guaifenesin, 3-(2-methoxyphenoxy)-1,2-propanediol 2 undergoes spontaneous resolution upon crystallization. This fact is confirmed by thermal analysis (single eutectic V-shape binary melting phase diagram, adequate entropy and free energy characteristics). Racemic 2 could be effectively resolved into (S)- and (R)-2 by a preferential crystallization procedure. Single enantiomer drugs levomoprolol and levotensin were obtained by starting from enantiomeric 2 through the sulfite route. |
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