Abstract
The terminology of “organocatalyst“ discussed in this chapter refers to small chiral organic molecules that catalyze and facilitate asymmetric transformations. The chapter describes two recent applications namely preparation of telcagepant, an application of iminium organocatalysis and preparation of MK-8613, application of asymmetric Michael addition catalyzed by desmethyl quinidine of organocatalysis on an industrial scale at Merck, and also addresses solutions to development issues encountered, from the lab scale to the industrial scale. The idea of what constitutes “large scale” is subjective, but in this context, the industrial scale refers to reactions that have been demonstrated on pilot plant scale and above. Overall, asymmetric organocatalysis is a useful tool in organic synthesis on large scale. Novelty and diversity resulting from the chemistry of asymmetric organocatalysis still continue to expand, and the application of organocatalysis will likely be much broader in the pharmaceutical industry in the future.
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