Forschungs- & Entwicklungsinformationsdienst der Gemeinschaft - CORDIS

Periodic Report Summary 1 - COSSHNET (Complementary Synthetic Strategies toward Heterocyclic Boronates)

COSSHNET is a dual-partner Industrial Doctorate (EID) offering research training in state-of-the-art chemical synthesis, catalysis, bioactive molecule design and high throughput library synthesis. Through integration of the complementary, interdisciplinary and intersectorial expertise of the partners, this network will help to strengthen Europe’s human resources in the fine chemical and pharmaceutical industries. The researchers will be supervised and mentored by internationally recognised experts and have access to state-of-the-art equipment. Hands-on training will be supplemented by formal training courses in relevant and related fields, and a wide variety of complementary training courses, summer school and seminars. Researchers will benefit from secondments to the industrial partner for a significant period of the project, thereby gaining extensive exposure to a commercially based scientific environment. Overall, it is anticipated that the COSSHNET project will provide both Early Stage Researchers (ESRs) with an outstanding training experience, through extensive technical and complementary skills development.

Overview and overall objectives:
The proposed dual-partner Industrial Doctorate will bring together expertise from the Harrity group at the University of Sheffield and the global healthcare leader Sanofi to make available a selection of technologies for the discovery and chemical synthesis of new small molecule entities. Small bioactive molecules will continue to play an important role in addressing areas relating to health and food security that are of critical concern to the EU, it is important that new actions are developed that support and grow the knowledge base in this area.
Traditionally, the Fine Chemicals sectors have favoured the design and development of heteroaromatic compounds. Therefore, one aspect of this activity will take advantage of classical medicinal chemistry concepts to provide a platform for new advances in these areas based on well-established principles. However, taking inspiration from the biological profile of natural products, the chemistry community has also begun to explore lead compounds bearing multiple sp3-centres and complex stereochemistry. A second and complementary activity will therefore focus its small molecule innovation areas towards the synthesis and functionalization of complex heterocyclic compounds. Accordingly, the projects carry significant opportunities to develop areas relating to catalysis and flow chemistry techniques. With respect to the latter, we have significant input from Sanofi who have state-of-the-art expertise and infrastructure in flow chemistry that promises to generate target molecules using faster and cleaner reaction processes with the potential for simple scale-up protocols.
Project website:

Progress and results
Both ESRs have begun to develop new synthetic methods towards heterocycles of value to the pharmaceutical industry. Specifically, an ynone condensation strategy has successfully delivered pyrazole and thiophene boronic acid derivatives, allowing a wide range of hetereoaromatic products to be made available through established cross-coupling chemistry. Moreover, an electrocyclisation method has been discovered that generates highly functionalised pyridines. Both ESR projects are therefore progressing well towards the stated objectives. Moreover, and through guidance from our partners at Sanofi, these techniques are being refined to allow easy incorporation of sp3-rich heterocyclic motifs. In this way, these complimentary synthetic methods appear to enable the delivery of a wide range of small molecule scaffolds. The potential of both methods to deliver small libraries of lead-like molecules will be assessed during the secondment at Sanofi.

Expected Results
COSSHNET will achieve its goals by recruiting 2 ESRs within a network of world leading academic and industry based partnerships from two member states in the EU. The ESRs will work on specific topics, developed collaboratively by the supervisory teams. It is envisaged that the proposed action will prepare the ESRs for effective independent careers within academia or industry, with strong appreciation of the challenges facing both sectors.

COSSHNET will deliver benefits at the European level in two principal areas; through contributions to the objectives of the European Research Area (ERA) and improving the scientific understanding in support of European policy. The scientific themes and objectives of COSSHNET will help to address research priorities in the Suschem European Technology Platform. COSSHNET will contribute to the research needs identified in this Suschem theme by: (i) improving the efficiency of synthetic routes to functionalised heterocyclic compounds through smart synthesis design; (ii) the introduction of new transition metal catalysed cyclisations for the regio- and stereoselective synthesis of drug-like functionalised intermediates; (iii) introducing new reaction platforms and media by the exploitation of high throughput and flow methods.
Overall, the proposed action will provide a platform for a new generation of young European scientists to further develop this exciting field through the collaboration of a network with expertise in the design and synthesis of new functionalised heterocycle scaffolds and their employment in drug discovery.

Reported by

United Kingdom


Life Sciences
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