Always Better To Go One Step Further

It has been acknowledge that enantiomers of drug substances produce significantly different pharmacokinetic and pharmacological activities. For this reason finding an efficient way of separating them has become an important aspect in the drug discovery process.

It is often considered that an asymmetric synthesis is the best route to pursue. However this can be costly. The purchase of enantiomerically pure starting material/ intermediate and synthetic expertise required can be very costly.

Over the last 25 years chromatography has come to the fore in delivering accurate measurement of enantiomers and a solid source of isomer isolation. With the correct screening protocol and breadth of selectivity space it is very easy to find conditions to separate enantiomeric pairs. Most separation scientists, especially from Large Pharma and CROs, have normal phase and polar organic chiral HPLC screening in place. The literature quotes around 80% success rate using this procedure. The next tier of instrumentation/technique expansion for separation scientists tends to be SFC. Again using an appropriate range of Chiral Stationary Phases (CSPs) the literature also quotes in the region of 80% success rate. Combining these techniques can bring success up to around 96%

The advantages of being a dedicated chiral purification service means that we have the time, equipment and expertise to challenge that final 4%. In attempting to do this we have found an underutilized technique to be very successful. Reverse Phase Chiral Chromatography has proven to be a very useful addition to our chiral screening service. On several occasions it has been the only technique which has shown a separation.

With all of these screening options available to us almost all enantiomeric separation challenges can be overcome.

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Final sample manipulation is sped up by our Biotage V10, allowing us to return samples within the same week!…