The development of concise, multi-kilo scale asymmetric syntheses of drug candidates, including the antiviral agent Letermovir will be described. The process features an asymmetric aza-Michael reaction as the key stereo-determining step, for which new cinchonidine-based PTC and Brönsted acid catalysts have been developed utilizing accelerated HTE methods. The general utility and efficacy of this reaction will be highlighted in the context of this and related substrates, together with current mechanistic understanding

Asymmetric synthesis of drug candidates: Discovery and development of novel aza-Michael catalysts for the synthesis of Letermovir

253rd National Meeting (2017)

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