Development of innovative synthetic processes for the industrial production of APIs

Active Pharmaceutical Ingredients (APIs) are a fundamental class of chemicals due to their important role in the human health. APIs are protected by intellectual property (IP), allowing the owners of the newly invented drug to have a temporary but complete exclusivity in terms of use, production and commercialization. The activity of the PhD is focused on the research of efficient and alternative synthesis of APIs, for which product/process patents are no longer valid or they are about to expire. The molecules selected for the research of alternative syntheses were vildagliptin (treatment of type 2 diabetes mellitus), fexofenadine hydrochloride (therapy for allergic rhinitis) and ravidasvir hydrochloride (a novel API, not yet approved, for the treatment of chronic hepatitis C). The aim of this work is to design alternative preparations for these selected APIs, optimising all the synthetic steps by adjusting reactions conditions and maximizing the yield of the processes and finally scaling up the whole syntheses to transfer the processes to the industrial scale.