In this project, we focus on target compounds, selected based on their challenging structure and potential for novel biological activity. We devise and execute the first complete synthesis of newly-discovered compounds and evaluate their activity in biomedical applications.

Having identified a compound with potential activity, we design analogues and build focused compound libraries with improved properties, for screening through a range of international collaborations.

Synthetic methods are pillars of chemical synthesis. We develop efficient, selective and environmentally benign reactions that have applications to pharmaceutical targets, specialty and fine chemicals. C-H activation, carbon-carbon and carbon-hetero bond formation, oxidation and reduction are under investigation. For example, in collaboration with Mitsui Chemicals, we have developed highly enantioselective hydrocyanation reactions of carbonyl compounds and imines for the synthesis of optically active cyanohydrins and a-aminonitriles which are general purpose chiral intermediates for pharmaceutical and fine chemical synthesis. This project has led to several patents and high impact publications.

Our research in route selection and process chemistry focuses on fine chemicals and pharmaceutical products, especially, atom economy, waste minimisation and environmental issues. The research is carried out in association with our Process Science and Modelling programme and our industrial partners. This is exemplified by our collaboration with Shionogi & Co. Ltd on the development of an alternative synthesis of Tamiflu in which inexpensive and abundant D-ribose is used as an alternative starting material. The work was highlighted by the American Chemical Society, Science Daily, A*STAR Research Publication and cited by several other media.

Lead identification and optimisation are two key stages of drug discovery where molecules with promising biological profile are identified for further development. We work closely with researchers from biomedical research institutes within A*STAR and drug discovery organisations internationally to identify and optimise lead compounds in cancer, infectious tropical diseases and neurodegenerative diseases. For instance, in collaboration with the Genome Institute of Singapore, we have developed several highly potent lead compounds for epigenetic cancer therapy. These compounds are now being investigated further in animal studies.

Specialty chemicals have designed properties that are crucial to the performance of a product. They are generally produced in small volumes but are highly value-added products. Flavours and fragrances, adhesives, water treatment agents, antioxidants, dyes, lubricants, pigments are the examples. In partnership with other research programmes within the institute, we develop chemicals with tailor-made properties and provide chemistry support to local and international chemical companies. For example, in conjunction with the Tropical Marine Science Institute at NUS and the Maritime Port Authority, we have successfully developed a series of environmentally benign, organic antifoulants for marine coatings. In collaboration with a chemical company, we are assessing the efficacy of these additives in commercial marine paints.