As a medicinal chemist, I am sure you would appreciate the simplicity of design. Here is an excellent example of an antiviral drug used in treating Hepatitis B, Tyzeka (Telbivudine). It is “just” the L-isomer of thymidine-that is it. The drug was marketed by Novartis (licensed from Idenix, a company was bought out by Merck in 2014). It relived the disease burden in thousands and thousands of patients, and generated millions of millions of dollars since its approval in 2006. Thanks to the discovery from Professor Jean-louis Imbach and Dr. Gilles Gosselin’s joined CNRS lab at the University of Montpellier. Their many years of sustained efforts in bioactive molecular chemistry culminated this life saving medicine. What I like here is not only the beauty of product but also the synthetic chemistry to make the drug. Smart application of silicon chemistry (my personal favorites) was a special feature in this paper published in the year 2000 including the use of silicon protection and the use of (TMS)3Si-H as a reducing agent (radical chemistry). Simplicity does not mean simple, Telbividine’s optimized semi-large scale synthetic sequence has near10 steps from L-Ribose (it’s not the natural D-Ribose).
