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A Large-Scale Synthesis of Enantiomerically Pure Cetirizine Dihydrochloride Using Preparative Chiral HPLC

โœ Scribed by Pflum, Derek A.; Wilkinson, H. Scott; Tanoury, Gerald J.; Kessler, Donald W.; Kraus, Hali B.; Senanayake, Chris H.; Wald, Stephen A.

Book ID
111933156
Publisher
American Chemical Society
Year
2001
Tongue
English
Weight
68 KB
Volume
5
Category
Article
ISSN
1083-6160

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Enantiomerically pure cetirizine can be prepared by preparative HPLC separation of cetirizine amide. The amide has an r value of 2.76 (USP resolution of 8.54) using a Chiralpak AD column, and 0.5 wt % of the amide (based on packing material) can be injected per run.

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## Racemic gossypol is resolved by HPLC of its amino acid ester Schiff's base derivatives on non-chiral columns. This provides a rapid and accurate method for determination of optical purityon a small scale and, combined with hydrolysis and fractional crystallization, for the preparation of pure g