SP Process Development AB Boosts Its Catalyst Screening with Chemspeed’s CATSCREEN 96

“The Chemspeed CATSCREEN 96 is a real workhorse with a capacity to run many hundreds of reactions per week. It enables us to rapidly generate and evaluate large numbers of catalysts for important transformations such as asymmetric hydrogenations and cross-couplings”, Dr. Per Ryberg, Senior Scientist Catalysis, from SP Process Development states, “Thanks to its unique capabilities, reliability and ease of use, the CATSCREEN 96 enables us to run entire sequences involving: generation of catalysts from precursors, addition of substrates / reactants, reaction at up to 80 bar pressure and sample preparation, fully automated and unattended. We use it for both catalyst screening and reaction optimization and work that would take several weeks to do manually can be done in a few days on the robot.”

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High Throughput Screening of a Catalyst Library for the Asymmetric Transfer Hydrogenation of Heteroaromatic Ketones: Formal Syntheses of (R)-Fluoxetine and (S)-Duloxetine

Elina Buitrago, Helena Lundberg, Hans Andersson, Per Ryberg, Hans Adolfsson

A total of 21 amino acid based ligands including hydroxy amide, thioamide, and hydroxamic acid functionalities, were combined with [Ru(p-cymene)Cl] and [RhCp*Cl], and used as catalysts for the asymmetric transfer hydrogenation of four different heteroaromatic ketones in 2-propanol. The reactions were performed on a Chemspeed automated high-throughput screening robotic platform. Optimal catalysts were identified for the individual heterocyclic substrate classes. Based on these results, the formal syntheses of the antidepressant drugs (R)-fluoxetine and (S)-duloxetine were conducted using these optimum catalysts in the key step, which results in high isolated yields (94 %) and excellent product enantioselectivities (>99 % ee) of the 1,3-amino alcohols.

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June 10, 2013