The authors surveyed the publications in three medicinal chemistry journals in 2008 covering 139 papers describing the synthesis of 3566 compounds and employing 7315 different reactions. They categorised the reactions that had been used and identified surprising trends such as the frequency of C-C bond forming reactions being about 10 %. They highlight the 10 most frequently employed reaction types (Table below) and that an average medicinal chemistry synthesis used 4.8 steps per compound (Graph). They finish with some challenges to chemists working in industry and academia.
For what happens when AI comes to reaction analysis see our next post…..
“The medicinal chemist’s toolbox: an analysis of reactions used in the pursuit of drug candidates” by Roughley and Jordan.
J. Med. Chem.(2011),54,10, 3451-3479
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