Crystalline pharmaceutical and methods of preparation and use thereof

摘要

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.;

主权项

1. A composition comprising an isolated compound of Formula I: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: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.