Summarization of Screening Hits

Summarization of Screening Hits on the Whelk-O^® 1, RegisPack^®, and RegisCell^® Chiral Stationary Phases

Introduction

The determination of enantiomeric purity is crucial in new drug development. The number of diverse chiral compounds is increasing and sensitive chiral methods are often needed quickly. Many new chiral stationary phases (CSPs) are available on the market making it challenging to select the most important ones for the initial screening stages and expedite method development. The focus of this study is to evaluate high selectivity Regis CSPs and to suggest the best screening method with a limited number of high success rate chiral columns.

Experimental

One thousand, one hundred sixty test compounds were screened on number of different CSPs. These were client-submitted samples for Regis’ free chiral screening service. The test library consisted of active pharmaceutical ingredients, potential drug candidates, proprietary research compounds, and commercially available compounds.

While we decided to summarize results for all the samples screened, a number of these compounds are unique and there is no guarantee that they are truly chiral.

The focus was on three of the most versatile columns on the market. They consist of the Whelk-O^® 1, RegisPack^®, and RegisCell^® CSPs. These three phases show a high success rate and broad versatility. In addition, these three CSPs are complementary in selectivity, as demonstrated by the number of unique hits for each CSP. All the columns were of standard dimensions, 25 cm x 4.6 mm i.d., packed with 5 micron particles. Each compound was screened individually and a number of different mobile phases were applied during the screening process to achieve optimal separation.