Advances in Eco-Sustainable CO2 Technologies

PIC Solution brings together SFC thoughts leaders to demonstrate the critical roles of SFC and SFE in the isolation of chiral/achiral Small Molecules, Peptides and Natural Products including Cannabis/Hemp. Technology enhancements to optimize instruments performance, increase throughput, reduce costs and minimize environmental impact will be also covered.

17:30 Separation of chiral compounds via SFC to support Genentech’s Drug Discovery Programs

Many molecules are developed and evaluated during early stages of drug discovery. The objective of Medicinal chemists is to design and synthesize molecules that will not only bind with high affinity to the target protein active site but also have good physicochemical properties. To achieve this objective, these molecules will often have one or more stereo-centers and the pure stereoisomer of interest will need to be isolated for testing, development, and regulatory approval. Genentech’s Analytical Research group has developed an optimized chiral screening workflow that utilizes a set of 15 chiral phases. This chiral screen uses short columns, short run times, and high flow rates to achieve rapid, high quality results. This approach has enabled us to rapidly screen and then scale-up to purify milligram to multi-gram quantities of chiral molecules in support of our drug discovery programs.

Presenter: Mengling Wong (Senior Scientific Manager, Genentech Inc.)

Mengling Wong is a Senior Scientific Manager at Genentech, Inc. in South San Francisco, CA. She leads a dynamic group supporting early research in Discovery Chemistry. She has over 19 years of experience in HPLC and SFC separations from small molecules to peptides. She received her Biochemistry degree from University of California, Davis. Besides supporting the drug programs at Genentech, she is also a member of the advisory board for the Green Chemistry Group and a Board of Directors on Enabling Technology Consortium. She has co- authored numerous papers on SFC and method development. Furthermore, she has presented at multiple conference venues with focus on improving preparative workflow and separations.

18:00 SFC support to Medicinal Chemistry and Chemical Process Development from mg to kg

To support Medicinal Chemistry and New Process Development projects in Pharmaceutical R&D, day after day, numerous intermediates or potential Active Pharmaceutical Ingredient (API) candidates are synthesized. The chemistry and isolation steps are rarely optimized and chromatographic purification steps are needed to timely delivered the compounds of interest. In UCB the well-established liquid purifications are performed for almost 30 years. At a prep scale, Reverse Phase (RP) on C18 or Normal Phase (NP) on silica are generally made based on the amount to purify, on the compound’s polarity, and taking into account chemistry’s constraints. Over the past 10 years, the SFC purifications became more and more considered and applied to get orthogonality with HPLC, to perform 24/7 process for very large scale and to decrease the amount of solvent to evaporate. This talk will be the opportunity to consider the strategy developed over the years to quickly purify different type of samples by choosing the right stationary phase for the right purpose or by choosing between HPLC and SFC. With regards to the chiral separations, some study cases will be presented to highlight the importance of the columns screening, the solubility of the samples and to compare SFC with Multicolumn Continuous (liquid) Chromatography process.

Presenter: Antoni Severino, Ph.D. (Head of Preparative Chromatography, UCB Pharma)

Antoni completed a PhD in Chemical Engineering at the University of Mons in Belgium in 2012. This thesis entitled “Experimental Study, Dynamic Modeling and Optimization of the Operating Conditions of Chromatographic Separation Processes by Simulated Moving Bed (SMB)” was funded by the Belgian National Fund for Scientific Research – FNRS. “Head of Preparative Chromatography” at UCB Pharma (Belgium) for almost 7 years, he is in charge of the Purification and Chiral separation Platform within Global Chemistry Research Department. His group supports Research in Belgium and UK but also the Development and the Manufacturing for MCC (Multicolumn Continuous Chromatography) processes. From mg to kg, the group deals daily with HPLC and SFC equipment for crude purifications, impurity isolations and chiral analyzes and separations.

18:30 Implementation of Supercritical Fluid Chromatography for the Concentration and Isolation of Cannabinoids from Hemp Extracts

The 2018 Farm Bill has opened many opportunities associated with the hemp plant. While cannabidiol (CBD) has shown promising health benefits, new opportunities to access minor cannabinoids have emerged. Minor cannabinoids such as Cannabigerol (CBG) and Cannabichromene (CBC) can be accessed directly from the plant through various breeding programs, while minor cannabinoids such as Cannabinol (CBN) are accessed through manipulation / degradation of CBD. As new cannabinoids like CBN emerge on the market, the responsibility of manufactures must increase in order to create safe products. Here we will discuss the utility of Supercritical Fluid Chromatography (SFC) for the isolation of hemp-derived cannabinoids.

Presenter: Eric Kawka (Founder and CEO, Cattis LLC)

Eric Kawka is driven to establish scalable extraction and purification methods for a new class of Cannabis derived products that meet pharmaceutical standards. Merging his background in analytical and organic chemistry with years of laboratory experience, he excels at developing production process-trains that maximize efficiency while maintaining product safety and reliability. Eric has significant experience with extraction and purification systems development, start-up ventures, and business management. Eric is an advisor for Cannabis start-ups in Vermont, Pennsylvania, West Virginia and Washington.

19:00 Leveraging Supercritical Fluid Chromatography for Some Unusual Application

This presentation will highlight developments in SFC technology that have opened new opportunities to impact Medicinal Chemistry projects. One example will describe how sample counterion equivalents can be quantitated rapidly with minimal sample usage using ELSD technology. Another application will demonstrate several unique characteristics of SFC chromatography, which enable the development of a methodology for measuring intra-molecular hydrogen bonding differences between matched pairs of compounds.

Presenter: Bill Farrell (Associate Research Fellow, Pfizer Inc.)

William Farrell is Associate Research Fellow at Pfizer Global R&D - La Jolla. Mr. Farrell received his BS degree from SUNY Stony Brook and has over 30 years chromatographic experience, specializing in supercritical fluid (SFC) and high pressure liquid (HPLC) chromatographic techniques. He has spent the last 20 years working on the implementation of SFC and HPLC for the analysis & purification of medicinal and combinatorial derived compounds. He has been a major driving force behind the development of automated Preparative SFC systems and has pioneered the use of SFC for high throughput applications for which he received the first annual Averica Award for his contributions to Preparative SFC and the ACS Technical Achievement in Organic Chemistry (TAOC) award. Current research areas include expanding SFC applications into biological systems and the development of novel, SFC specific stationary phases.

19:30 PIC Solution Latest SFC, SFC-MS and SFE Innovations

An overview of the novel technologies developed by PIC Solution with a focus on the newly designed Open-Bed SFC-MS and high-through analytical SFC systems (2-5 columns in parallel) will be discussed. The Open-Bed SFC-MS enhances the eco-friendly and sustainability benefits of SFC with CO2 recycling in Open-Bed mode and capabilities to conduct separation in the low mg scale.

Presenter: Gerard Rosse, Ph.D. (Vice President North America, PIC Solution Inc.)

Dr. Rosse is Vice President, North America, at PIC Solution Inc. He received his BS and his Ph.D. in Chemistry from the University of Basel, Switzerland, and did postdoctoral studies at Stanford University, California. Dr. Rosse has extensive experience in analytical chemistry, medicinal chemistry and drug discovery working with F. Hoffmann-La Roche, Sanofi, Cephalon and Dart NeuroScience. Most recently, he pioneered the implementation of SFC-MS at research and industrial scale to support small molecules automated synthesis reaching 90,000 compounds per year and reducing significantly production costs. Dr. Rosse is the author of many publications, patents and presentations, and recently edited a book on modern SFC applications.