Annual Spring Symposium Day 3

with Katherine Lainhart, and Deirdre Cabooter
Thursday, April 15, 2021
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About This Meeting

The theme of this year’s virtual event is Advancing Chromatorgaphy in Industry . 

The event will take place over the lunchtime hour of 12:00 – 1:00 p.m. on April 13, 14, & 15, 2021.

There is no cost for the event this year due to its virtual nature so this is a perfect time to enjoy the science being shared, as well as get an inside look at the CFDV, one of the longest running chromatography organizations in the country.

 

11:45 am Event log-in opens
11:50 – 11:55 am Welcome message from CFDV
11:55 am – 12:00 pm PerkinElmer presentation
12:00 – 12:30 pm “Analysis and Control Strategies for Boron-Containing Intermediates in Small Molecule Drug Substance Processes” Katherine Lainhart, BMS

12:30 – 1:00 pm “Analytical tools to monitor environmental micropollutants and their degradation products in water: advances in liquid chromatography” Deirdre Cabooter, KU Leuven

 

“Analysis and Control Strategies for Boron-Containing Intermediates in Small Molecule Drug Substance Processes”
Katherine Lainhart, BMS

Abstract: With the wide adoption of transition metal-catalyzed cross couplings over the past decades, the use of boron-containing materials as intermediates and starting materials in drug substance processes has become more prevalent throughout the pharmaceutical industry, especially in early phase clinical development. Whether using boronic acids or their corresponding boronate esters, creating a robust analytical method for boron-containing materials is often challenging. Boroxines and other various anhydrides that originate from the facile dehydration of boronic acids convolute quantitative testing. Boronate esters readily undergo hydrolysis in aqueous conditions, complicating reverse phase chromatographic methods. Furthermore, boron-containing compounds are frequently flagged as potentially mutagenic impurities, necessitating tighter control of the residual levels in the final drug substance. This talk will discuss two boron-containing intermediates and the strategy for their release testing and control of residual boron-containing impurities downstream in the synthetic process.

 

“Analytical tools to monitor environmental micropollutants and their degradation products in water”
Deirdre Cabooter, KU Leuven

Abstract: The discharge of organic micropollutants (OMPs), such as pharmaceuticals, pesticides, personal care products,hormones, etc., in waste and surface water and their effects on the environment have recently become a topic of great concern. These OMPs are disposed in the environment via human and animal excretions, agricultural processes and industrial activities. Effluents from households and hospitals are typically treated in wastewater treatment plants (WWTPs). The current generation of WWTPs is, however, not designed to remove these OMPs, which can hence largely
pass the WWTPs unaffected. This has resulted in environmental concentrations in the ng/L to µg/L range for a plethora of OMPs, where they can exhibit a negative effect on aquatic organisms. It is clear that the presence of these OMPs needs to be monitored carefully, and adequate techniques for their removal are in order. Such removal techniques consist for example of membrane bioreactors and activated carbon, nanofiltration and advanced oxidation processes (AOPs). Some of these techniques can, however, lead to the creation of secondary waste (streams) or the production of degradation and
transformation products that can potentially be more toxic than the original parent compounds. In this presentation, an overview is given of different studies our teams have recently undertaken to deal with the problem of emerging OMPs in the environment. A novel liquid chromatography (LC) solution that couples orthogonal separation mechanisms, such as hydrophilic interaction liquid chromatography (HILIC) and reversed-phase liquid chromatography (RPLC), in series using a single pump is presented as a robust solution for the analysis of a large number of compounds with a wide variety in polarity, such as OMPs and their degradation products. High-resolution mass spectrometry is used to identify degradation products that are created using different types of chemical degradation techniques. Finally, zebrafish larvae are presented as an in vivo model to determine the toxicity of the OMPs and their degradation products.

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