Floris Rutjes - Biography#

Prof. Rutjes is an internationally renowned expert in the synthesis of organic small molecules. Over the years he has developed several important new directions in this field of research, including (i) New Synthetic Methods, i.e. the development of new catalytic and sustainable synthetic routes to organic compounds, (ii) Medicinal Chemistry, i.e. the synthesis of small molecules with biological activity, (iii) Molecular Bioconjugation, i.e. fast, so-called “click” probes, for applications in biology, and (iv) Flow Chemistry, i.e. chemical synthesis in continuous flow microreactors. As to (i) and (ii): he has combined chemo-enzymatic and transition metal‐catalyzed reactions to synthesize enantiopure functionalized heterocyclic building blocks and natural products. More recently, he has combined multiple (incompatible) catalysts to create complex multi‐step processes in one pot. To this end he has used various types of catalysts (enzymes, metal catalysts, organocatalysts) in one reactor or in compartmentalized reactors using e.g. polymersomes or immobilized reagents to physically separate incompatible catalyst systems. In connection with (iii) he has designed, synthesized and applied bioconjugation (click) probes for use in chemical biology research. Two of the globally most often used click-probes – strained cyclooctynes, termed BCN and DIBAC/DBCO – have been developed in his group and were brought to the market by him and are currently applied in clinical trials in antibody-drug conjugates, so-called ADCs. Furthermore, he has established a name world-wide with his research on the use of continuous flow microreactors in organic synthesis (item iv). He is one of the pioneers in this field and explored their use when the microreactor field was still in its infancy. In collaboration with the Fraunhofer Institute in Duisburg, Germany, and with Prof. Jan van Hest, from Eindhoven University of Technology, Eindhoven, The Netherlands, he has constructed a very versatile plug‐and‐play microreactor platform. It was used to develop new approaches for conducting organic chemistry reactions, ranging from inherently safe processes involving hazardous reagents, to catalytic continuous flow reactions, and further to large scale photochemical processes.

The great strength of Floris Rutjes is his open eye for applications. He cleverly connects fundamental academic research with industrial applications. In this connection he has been very successful in coordinating multidisciplinary research teams. In May 2020, he was awarded a grant (1.5 M€) by the Top-sector Health-Holland program in The Netherlands to lead a consortium (2 companies and several groups from Academia) to develop antiviral compounds against COVID-19. He is also part of an international EU-Eurostar-funded consortium (led by the Swiss Pharma company Addex) to develop small molecules against the disease Post-Traumatic Stress Disorder (PTSD). A recent project that he is leading concerns the “Center for Open Innovation in LEad Discovery (COILED)”, a European EFRO-funded project jointly carried out with research groups from the Radboud University Medical School, Pivot Park Screening Center in Oss, and scientists from the former Pharma Company Organon. This is a multidisciplinary project in the field of medicinal chemistry, aiming at the development of new lead compounds for societally relevant biological targets in the field of innate and trained immunity, which has led to new series of highly potent unique small molecule compounds. Another recent example is the large collaborative and multidisciplinary project termed UltraSense, which he coordinated. In this project a consortium of academic researchers in organic chemistry, solid state/liquid NMR, microfluidics, MRI imaging, and industrial researchers from 4 different companies study how chemical compounds can be rendered more sensitive for detection by NMR through (reversible) reaction with para‐hydrogen (SABRE-hyperpolarization). Besides being involved in research, he also likes to stimulate the exploitation of scientific inventions for further applications in society. The enzymatic technology that he developed, formed the basis for founding the spin‐off company Chiralix (2002), which was later acquired by Symeres (formerly Mercachem company). The combination of his unique flow chemistry knowledge and proprietary hardware served as a basis for the spin‐off company FutureChemistry (2008), which became a prominent player in the microreactor synthesis field, currently focusing on flow applications for making radio-labelled compounds. Besides these two companies, it is worth mentioning that the spin‐off companies Synaffix (2010, founded by Prof. van Delft, who is currently affiliated with Wageningen University) on click‐chemistry, Pansynt (2012, antibiotic, antimalarial compounds), Protinhi (2014, founded by Associate Prof. Martin Feiters, antiviral compounds against Dengue, Zika) and COILED Therapeutics (2018, with Profs. Netea and Joosten from the Radboud University Medical School and Dr. Wijkmans, former employee of Organon company) on trained immunity, were founded based on fundamental research that was carried out under his guidance.

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