When Does Asymmetric Synthesis Make More Sense Than Chiral Resolution?

June 20, 2014

In this article Jeffrey Kiplinger, President and Founder of Averica, responds to the question “When does asymmetric synthesis make more sense than chiral resolution?”

Consider synthesis if it is fast and inexpensive, or if you know you have to get to a quantity that is greater than isolation can provide in a reasonable time for reasonable cost.

It’s always a balance between the costs of the two approaches.

Example 1 
A client wanted to develop a scalable synthesis that could go to GMP production for their compound, and they wanted to do the final enantiomer resolution by diastereomeric salt resolution. It cost them a lot of money and went nowhere. To keep their project timeline on track, they needed compound supply immediately.

Averica developed a fast and efficient separation.  The client decided that chromatographic resolution was the best solution for quantities up to about 200-500g. It has been a load off their mind that they don’t need to worry about whether they will achieve the GMP synthesis.

Example 2
A discovery scientist needed to make 20g of material for an animal study. He decided to pursue an asymmetric synthesis that would yield chirally pure/optically pure material. That synthesis could take up to 6 weeks to develop, depending on whether you get the desired material on the first try.  They tried it 4 times, only got to 75%, and spent 4-5 weeks doing it. That’s when they contacted Averica and asked if we could help, and help quickly because they already had animals scheduled.

Thinking about both approaches at the same time is the way to go.  Consider the advantages of both approaches before making your decision.

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