Catalysis has become increasingly important for the pharmaceutical industry. Catalysis is a critical technology that enables economical and environmentally-sound manufacturing processes. The development of a viable catalytic process for industrial scales is a complex task that requires the collaboration of multiple disciplines. In this article, a number of selected, noteworthy industrial examples are discussed to showcase the catalytic technologies that have been successfully practiced on large scales for active pharmaceutical ingredient (API) synthesis, involving transition metal catalysis, biocatalysis and organocatalysis. In addition, several examples of potential and future catalytic transformations are included which can be utilized in pharmaceutical industry in large-scale operational settings.

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As pharmaceutical API projects advance from Development to Chemical Production, the primary objective of the Process Research and Development (R&D) chemists is a smooth transfer of a well-developed, safe, scalable, robust, and economical chemical process to their customers in Chemical Production. Since the definition of a Good Chemical Manufacturing Process differs widely amongst different departments and companies, we herein summarize eight useful process evaluation criteria, and then demonstrate our deployment according to the guiding principle “if it can be measured, then it can also be managed”, with the aim to offer chemists a helpful toolbox to effectively compare competing API synthesis routes.

N-Heterocyclic carbenes were found to be highly effective organocatalysts in activating TMSCN for facile cyanosilylation of carbonyl compounds. Cyano transfer from TMSCN to aldehydes and ketones proceeds at room temperature in the presence of only 0.01-0.5 mol % of N-heterocyclic carbene (1), leading to a range of trimethylsilylated cyanohydrins in very good to excellent yields. These conditions are extremely mild and simple and tolerate various functional groups.

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