54th Organic Process Research and Development Conference

Streamlining Early Phase Drug Development with Continuous Flow Technologies

I earned my bachelor’s and master’s degrees in chemical engineering from Laval University (Quebec City, Canada) in 1996 and completed a doctoral degree in heterogeneous catalysis at the University of Technology Aachen (Germany) in 2001. I joined Lonza in March 2001 as a Laboratory Head for reaction engineering and safety assessment. In February 2003, I became the Project Leader for Lonza’s Microreactor Technology until July 2007. I then served as an Associate Professor at the University of Ottawa from August 2007 to July 2008. Returning to Lonza in September 2008, I focused on continuous-flow technology and business development from 2009 to 2012. From 2013 to 2023, I was Director and Head of an R&D group in API Chemical Services, and since 2024, I’ve led the Advanced Chemistry Technologies group. I also supervise graduate students as an Adjunct Professor at the University of Ottawa, with their practical work done in Visp, Switzerland.

PharmECO: Sustainable Chemical Processing Using Flow Technology

Professor C. Oliver Kappe received his diploma- (1989) and his doctoral (1992) degrees in organic chemistry from the University of Graz where he worked with Professor Gert Kollenz on cycloaddition and rearrangement reactions of acylketenes. After periods of postdoctoral research work on reactive intermediates and matrix isolation spectroscopy with Professor Curt Wentrup at the University of Queensland in Brisbane, Australia (1993- 1994) and on synthetic methodology/ alkaloid synthesis with Professor Albert Padwa at Emory University in Atlanta, USA (1994-1996), he moved back to the University of Graz in 1996 to start his independent academic career. He obtained his “Habilitation” in 1998 in organic chemistry and was appointed Associate Professor in 1999. Since 2011 he holds the position of Professor of “Technology of Organic Synthesis” (Organische Synthesetechnologie) at the University of Graz. He has spent time as visiting scientist/professor at e.g. the Scripps Research Institute (La Jolla, USA, Professor K. Barry Sharpless, 2003), the Toyko Institute of Technology (Toyko, Japan, Professor T. Takahashi, 2008), the University of Sassari (Sassari, Italy, 2008), the Sanford-Burnham Institute for Medical Research (Orlando, USA, 2010) and the Federal University of Rio de Janeiro (Rio de Janeiro, Brazil, 2013).  The co-author of more than 300 publications, his main research interests have in the past focused on multicomponent reactions, combinatorial chemistry and the synthesis of biologically active heterocycles. More recently his research group has focused on the use of enabling and process intensification technologies for synthetic chemistry, including microwave and continuous flow processing.  For his innovative work in microwave chemistry he received the 2004 Prous Science Award from the European Federation for Medicinal Chemistry and the 2010 Houska Prize (€ 100.000) in addition to a number of other awards.

The Manufacture of MK-0616, a Large Small Molecule

Tiffany Piou is an associate principal scientist of Process Chemistry in the Process Research and Development organization at MSD. She obtained a M.Sc. in Chemistry from University of Paris-Orsay and she obtained her Ph.D. in Organic Chemistry under the supervision of Prof. Jieping Zhu at ISCN (Gif-sur-Yvette, France) and EPLF (Lausanne, Switzerland). She then moved to the US to conduct her postdoctoral research in the laboratory of Prof. Tom Rovis at Colorado State University and Columbia University where, she developed Rh(III) catalysts C-H activation reactions.  In 2017, she joined MSD in the Discovery Process Chemistry (DPC) team based in Rahway (NJ). During her time, she had the opportunity to contribute to discovery and development programs across multiple therapeutic areas, including oncology and Alzheimer’s disease. Over four years ago, she joined the Process Chemistry team working on MK-0616 manufacture.

Sustainability at AstraZeneca: The development and use of earth-abundant metal catalysis in Chemical Development

Scott obtained his MChem from the University of Leeds in 2017 under the supervision of Dr Visuvanathar Sridharan on the synthesis of MDM2-p53 inhibitors. He stayed on at the University of Leeds to carry out his PhD under the joint supervision of Professor Adam Nelson and Professor Steve Marsden, working on the synthesis of diverse sp³-rich molecular scaffolds for applications in medicinal chemistry. In 2021, Scott joined AstraZeneca as a postdoctoral associate, where he began investigating earth-abundant metal catalysed reactions as an alternative to traditional platinum group metal (PGM) catalysis using high-throughput experimentation, focussing primarily on borylation and Suzuki reactions. He is now a senior scientist at AstraZeneca, where he continues to work on base metal catalysed reactions with applications in process chemistry.

Collaborative Innovation in Pharmaceutical Development: Unleashing the Power of AI, Data Science, and Open Science Initiatives

Julius Hillenbrand leads Digital Process Chemistry within the CMC department at Bayer Pharmaceuticals. He studied Chemistry and conducted research at Ludwig-Maximilians-University of Munich, RWTH Aachen University, UC Berkeley, and the Max-Planck-Institute für Kohlenforschung in Mülheim. During his doctoral research, Julius developed an innovative class of catalysts for alkyne metathesis, earning recognition through the Thiel Award and the Otto Hahn Medal for outstanding scientific achievement from the Max-Planck-Institute and the Max Planck Society. Julius joined Bayer in March 2021, where he leads a team of highly experienced and educated lab scientists in process chemistry at the Wuppertal site. In this role, he is passionately driving initiatives to automate, digitize, and accelerate the optimization of chemical reactions through disruptive technologies and cutting-edge data science tools. In his seminar today, he will share valuable insights on this transformative approach to process chemistry.

Second-generation manufacturing process of Migoprotafib

Paolo Tosatti studied Chemistry at the University of Genoa (Italy), where he obtained his MSc in 2007, before moving to England to pursue a PhD at the University of Leeds in collaboration with GlaxoSmithKline. After this experience, he moved to Switzerland to join the group of Prof. Andreas Pfaltz at the University of Basel as a postdoc. There he worked in the fields of hydrogenations mediated by frustrated Lewis pairs and asymmetric catalysis. In 2013, Paolo started his career in industry joining Novartis Animal Health (later evolved into Elanco) as a medicinal chemist and research project leader. Five years later, he joined the Synthetic Molecules Technical Development department at F. Hoffmann-La Roche, where he is currently working as principal scientist and chemistry project leader, as well as responsible scientist for the hydrogenation laboratory. Main activities and professional interests of Paolo’s include asymmetric catalysis, hydrogenation and the development of safe, robust and efficient synthetic routes to active pharmaceutical ingredients, including their transfer to manufacturing scale.

Route scouting and route optimization for Elimusertib (BAY1895344)

Richard van der Haas obtained his Ph.D. from the University of Leiden under Prof. Johan Lugtenburg for the synthesis of porphyrin derivatives for photodynamic therapy applications. He then spent two years at the University of Amsterdam under Prof. Henk Hiemstra to investigate organocatalytic conversions with cinchona alkaloids and with chiral phosphoric acids. After his academic career Richard continued in Nijmegen at Symeres bv in 2007. After five years, he switched from synthetic chemistry to process R&D, initially as Senior Scientist, but from 2014 on as a Team Leader. In this role he got involved in many different process R&D related projects dealing with topics such as route scouting and optimization, catalyst- and condition screenings, impurity structure elucidation and impurity synthesis. Richard has been involved in a fruitful collaboration with Bayer AG for a long time. The presentation here is a showcase of this collaboration.

Advancing Metal-Catalyzed Reactions through Optimized Precursor-Ligand Combinations

Angelino completed his Master’s degree in Chemistry at the University of Sassari in Sardinia, Italy. Following this, he earned his Ph.D. in Chemistry from RWTH Aachen University in Germany, specializing in organometallic chemistry and homogeneous catalysis under the mentorship of Prof. Albrecht Salzer. In 2007, he joined Umicore Precious Metals Chemistry (PMC) as a Scientist in the Chemical Development Department. Since then, he has led teams in developing safe, economical, and robust processes for metal-based catalysts, from initial concept through to large- scale manufacture. His work encompasses a variety of applications, including metathesis, hydrosilylation, cross-coupling (CX), asymmetric hydrogenation, and more.

In 2024, Angelino was promoted to Principal Scientist. He now oversees the development of both precious metal and earth-abundant based catalyst portfolios, collaborating closely with university and industrial partners.

BASF’s super edge-coated precious metal catalysts

Bert received his M.Sc. degree in chemistry from the University of Nijmegen in 1996 followed in 2001 by his Ph.D. from the University of Amsterdam where he worked with Professor Piet van Leeuwen and Professor Joost Reek on the immobilization of homogeneous catalysts. After periods of postdoctoral activities at Cambridge University (triplet emission in semiconducting polymeric systems); Engelhard (heterogeneous catalysis) and the University of Amsterdam (commercial spin off activity developments) he joined BASF in 2009. After 4 years in R&D, developing a wide range of base- and precious metal catalyst recipes, he moved to the marketing team for Hydrogenation Catalysts, first as Marketing Manager and since 2018 as Technology Manager. His role is to understand and optimize the hydrogenation processes of BASF’s customers with cutting edge catalytic solutions. His presentation at the 54^th ORPD Conference in beautiful Lisbon will be about finding the sweet spot for supported precious metal catalyst formulations between metal usage efficiency and catalyst performance.

Iptacopan/Fabhalte: Development of a First-in-Class, Oral Factor B inhibitor

Dr. Simon Allmendinger is a Senior Scientist in chemical and analytical development at Novartis Pharma AG in Basel, Switzerland. Since joining in 2017, he was involved in both early and late phase development of small molecule APIs aiming at the optimization of chemical synthetic routes into efficient, safe, and sustainable processes. Exemplary, he was the leading chemist behind Iptacopan and supported the project until its regulatory approval for the treatment of PNH in 2023. Furthermore, he leads efforts to bring novel synthetic methodologies, including photochemical transformations, to industrial applications and supports the innovation management within the organization to help to initiate new projects within the strategic portfolio. Simon studied chemistry at the University of Basel before moving to the Albert-Ludwigs-University in Freiburg to pursue his graduate studies with Bernhard Breit, working on ligand design for the asymmetric hydroformylation. After a visiting scientist position at the ICIQ Tarragona, working with Kilian Muniz on I₂-catalyzed amination reactions, he moved to Princeton University to join Dave MacMillan’s group to explore metallaphotoredox-catalyzed Cross-coupling reactions.