Development and Application of a New Class of Halogenated Reagents to Commercially Valuable Targets

ended

The aim of this project is to expand upon a newly discovered platform reaction by developing new routes to Active Pharmaceutical Ingredients (APIs) Tolterodine and Ezetimibe and other advanced intermediates for the manufacture of drugs (i.e. benzylic fluorides and alcohols). It is planned that this platform will serve to enhance the competitveness of the European pharmaceutical manufacturing industry as it continues to face increased competition from other economies In order to achieve this aim we need to bring together expertise in (i) Organic Synthesis [Royal College of Surgeons in Ireland, “RCSI”] (ii) Enantioselective fluorination [Nagoya University Japan, “Nagoya”] (iii) Drug development and production [Integrated Research in Biotechnology & Medicine, “IRBM”] To meet the aim we have divided the project into the following work packages: WP1: Development of a new synthesis of Tolterodine. WP2: Scale up of synthesis of Tolterodine. WP3: Development of a new synthesis of Ezetimibe. WP4: Scale up of synthesis of Ezetimibe. WP5: Exemplification of alkoxylation to prepare enantiopure benzylic alcohols API intermediates WP6: Preparation of benzylic fluorides WP7: Management, Training, Dissemination & Communication