Researchers at Princeton University have introduced a long-awaited reaction capable of forming sp3-sp3 bonds whose presence increases a molecule’s complexity and its chances for clinical success as a drug candidate.
The study detailed a mild and general method to couple sp3 carbon atoms – carbon centers defined by that fact that only single bonds connect them to their neighbors. Until now, this coveted reaction had resisted chemists’ efforts, even eluding transition metal catalysis, a powerful field that has enabled a staggering range of coupling reactions over the past 50 years.
The reaction is a very unique way of approaching how you would join molecules together, and broadly expands the types of carbons you can connect.
The team demonstrated the reaction’s generality as it proceeded smoothly with array of structurally diverse partners. Using this method, they also constructed the antiplatelet drug tirofiban in two steps from simple starting materials using their sp3-sp3 coupling reaction and another metallaphotoredox method recently developed in their lab. This example showcased the utility of their program for drug discovery though it holds potential for other industries as well.
https://chemistry.princeton.edu/news/researchers-unlock-coveted-bond-connection
Study: http://www.nature.com/nature/journal/v536/n7616/full/nature19056.html
The study detailed a mild and general method to couple sp3 carbon atoms – carbon centers defined by that fact that only single bonds connect them to their neighbors. Until now, this coveted reaction had resisted chemists’ efforts, even eluding transition metal catalysis, a powerful field that has enabled a staggering range of coupling reactions over the past 50 years.
The reaction is a very unique way of approaching how you would join molecules together, and broadly expands the types of carbons you can connect.
The team demonstrated the reaction’s generality as it proceeded smoothly with array of structurally diverse partners. Using this method, they also constructed the antiplatelet drug tirofiban in two steps from simple starting materials using their sp3-sp3 coupling reaction and another metallaphotoredox method recently developed in their lab. This example showcased the utility of their program for drug discovery though it holds potential for other industries as well.
https://chemistry.princeton.edu/news/researchers-unlock-coveted-bond-connection
Study: http://www.nature.com/nature/journal/v536/n7616/full/nature19056.html