Boehringer-Ingelheim Lecture

Drug Substances are becoming increasingly complex and costly to manufacture, and development of sustainable processes is challenging. Asymmetric catalysis is attractive but efficiency and availability of the catalysts must be considered for process development. New technologies and methodologies for their synthesis are frequently needed. This presentation discusses our efforts on identifying and developing a general method for the synthesis of P-stereogenic chiral phosphine compounds, which was successfully applied in the production of P-stereogenic chiral phosphine ligands on large scale (J. Am. Chem. Soc. 2013, 135, 2474−2477; Angew. Chem. Int. Ed. 2015, 54, 5474 –5477; Org. Lett. 2017, 19, 1796−1799). The design and development of a practical process for the production of a chiral polycyclic CETP inhibitor via asymmetric catalysis will be also discussed (Org. Lett. 2014, 16, 4142−4145).