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Five minutes with Grazyna Szymanska, president – US branch, Apeiron Synthesis – DCAT Week ‘18

PH: Apeiron is basically about catalytic olefin metathesis, a technique that has been known for decades but without any major commercial application. Has it now come of age?

Grazyna Szymanska

Grazyna Szymanska

Szymanska: Yes, it has. The breakthrough came with the design of more specific and robust catalysts which made large-scale synthesis feasible. Boerhinger Ingelheim used the Nitro-Grela catalyst, our flagship product, to prepare the HCV inhibitor BILN 2061 for Phase II trials. This was the very first large-scale macrocyclisation carried out under practical conditions using olefin metathesis.

PH: What have been the major milestones Aperion has achieved in the last few years?

Szymanska: We introduced three metathesis screening kits to speed the identification of the most effective catalyst and reaction conditions for the task at hand, whatever it might be. All of the catalysts in them have robust stability and scalability. Successful metathesis conditions identified with these screening kits can be carried through to process optimisation, scale-up and production and the same catalyst will be available and effective at each stage of development.

PH: You are a Polish-based company, headquartered at Wroclaw. How do you address the US market?

Szymanska: We are very much embedded within the local ecosystem. Our US office is located at Cambridge Innovation Centre and we are a member of the Massachusetts Biotechnology Council. Two years ago, we launched the Catalysis in Chemistry Symposium there, bringing together global leaders in catalysis from pharma and academia, and we are present at all major US trade shows and conferences.

PH: Between 2012 and 2015 you introduced many new catalysts to the market. Since HeatMat in 2015, there have not been any others. Are there any new technology developments in the pipeline you can share with us?

Szymanska: We are continuously developing new catalysts to respond to new synthetic challenges. Since 2015, we have been working on new versatile ruthenium-based catalysts for olefin metathesis. This effort resulted in a new class of complexes called bis(CAAC)ruthenium indenylidenes that combine the benefits of the NHC and CAAC families. Currently we have three new catalysts available, either from Strem or directly from us. One of these, UltraCat, is extremely versatile and highly efficient in virtually all metathesis transformations leading to terminal and internal olefins, such as ethenolysis, ring-closing metathesis and cross-metathesis involving electron-deficient partners like acrylates, or ene-yne metathesis. These transformations take place with exceptionally low catalyst loadings and high selectivity. For example, in the self-metathesis of 1-decene, a turnover number over 300,000 was obtained.

PH: You also offer fine chemical manufacturing from grams to hundreds of kilos scale. How is business in that area now? Do you find that it complements your catalyst offering? And have you made any investments in this field lately? Do you have any planned?

Szymanska: Early this year, we opened a second site, a few miles away from our headquarters. It is equipped with high-end reactors which allows us to produce 500 kg of given catalyst.

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