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|Title:||Crystalline pharmaceutical and methods of preparation and use thereof|
|Abstract:||Novel crystalline polymorphic forms, Forms A, B, C, D, and E of a compound of Formula I, which has been found to be a potent inhibitor of LFA-1, are disclosed. Methods of preparation and uses thereof in the treatment of LFA-1 mediated diseases are also disclosed in this invention. ##STR00001##|
|Inventor(s):||Burnier; John (Pacifica, CA)|
|Assignee:||SARcode Bioscience Inc. (Brisbane, CA)|
1. A composition comprising an isolated compound of Formula I: ##STR00020## or a salt thereof, wherein said compound is synthesized according to a method comprising the
steps: a) performing base hydrolysis of Formula AA with a base in an aprotic solvent, or performing acid hydrolysis of Formula AA with an acid in an aprotic solvent: ##STR00021## wherein R is a carbon containing moiety; and b) isolating a compound of
Formula I or a salt thereof, with an enantiomeric excess of greater than about 90%; wherein said composition has a lower level of residual palladium compared to a composition comprising a compound of Formula I or a salt thereof prepared by
palladium-catalyzed transfer hydrogenolysis.
2. The composition of claim 1, wherein the aprotic solvent is dioxane.
3. The composition of claim 1, wherein the base is sodium hydroxide.
4. The composition of claim 1, wherein the acid is hydrogen chloride.
5. The composition of claim 1, wherein R is a substituted or unsubstituted group selected from lower alkyl, lower alkenyl, lower alkynyl, cyclo(lower)alkyl, cyclo(lower)alkenyl, aryl, aralkyl, heterocyclyl, and heteroaryl groups.
6. The composition of claim 1, wherein the residual palladium in the composition is less than about 100 ppm.
7. The composition of claim 1, wherein the residual palladium in the composition is less than about 50 ppm.
8. The composition of claim 1, wherein the residual palladium in the composition is less than about 10 ppm.
9. The composition of claim 1, wherein the residual palladium in the composition is less than about 1 ppm.
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