‘Late-stage saturation’ could improve drugs' effectiveness
Approach turns flat aromatic structures into three-dimensional saturated molecules with improved medicinal properties
A general and quick strategy for converting complex aromatic building blocks into saturated molecules with improved medicinal properties has been developed. The new approach – called late-stage saturation – opens up opportunities in drug discovery and drug optimisation.1
‘The production of new medicines depends on the synthetic availability of suitable molecular structures, which usually have to be built up in several reaction steps,’ explains Frank Glorius at the University of Münster in Germany who led the study together with Tim Cernak from the University of Michigan in the US and Jiajia Ma at Shanghai Jiao Tong University in China. ‘It is time-saving and attractive if advanced, drug-like building blocks can be diversified. We show that aromatic hydrogenation under mild conditions is suitable for this purpose.’