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Expanding the scope of HTS-driven development – applications to highly potent compounds and catalytic processes


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Current pressure on R&D budgets in pharmaceutical and chemical industry sets the trend for efficient tools in process development. In this context, access to high throughput experimentation (HTE) platforms is a key issue for the rapid and cost efficient development of active pharmaceutical ingredients (APIs). About 7 years ago, Solvias installed a fully integrated high throughput screening workflow designed by Symyx Inc. (now: Freeslate Inc.). In the meantime, Solvias has been establishing a global business for the efficient evaluation of catalysts for process development. Specifically, Solvias is offering screening solutions for homogeneous asymmetric hydrogenation, any type of metal catalyzed C-X coupling reactions, selected enzymatic reactions and crystallization studies. Recently, Solvias has devised two modified workflows that can handle heterogeneous catalysts and highly potent compounds on this platform. These two new achievements will be presented in this article.

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Heterogeneously catalyzed reactions such as hydrogenation on production scale are widespread in the life science and fine chemicals industry. The handling of airsensitive solids (catalysts) is a key aspect when developing such process. This task is also critical on small scale in combination with a high throughput experimentation platform, even though it is located in a glovebox under inert atmosphere. In addition to the screening of heterogeneous catalysts for generic activity and selectivity, it is highly desirable to perform kinetic experiments using the HTE platform. Such investigations only can be conducted when variable amounts of the heterogeneous catalyst(s) efficiently can be distributed on the reaction plate. Solvias has developed a technology that allows the rapid dosing of different levels of catalyst loadings. Almost every commercially available catalyst can be applied by means of ...