Streamlined Functionalisation of Nitrogen-containing Molecules by Palladium-catalysed C-H Activation

Project Information

ACTPD

Grant agreement ID: 747600

DOI

10.3030/747600

Project closed

EC signature date 22 February 2017

Start date 10 March 2017

End date 19 April 2019

Funded under

• EXCELLENT SCIENCE - Marie Skłodowska-Curie Actions

Total cost

€ 183 454,80

EU contribution

€ 183 454,80

Coordinated by

THE CHANCELLOR MASTERS AND SCHOLARS OF THE UNIVERSITY OF CAMBRIDGE
United Kingdom

Periodic Reporting for period 1 - ACTPD (Streamlined Functionalisation of Nitrogen-containing Molecules by Palladium-catalysed C-H Activation)

Reporting period: 2017-03-10 to 2019-03-09

Summary of the context and overall objectives of the project

Chemical reactions are highly valuable tools for scientists and for society since they provide useful materials not found in nature. The overall objective of the project is to develop novel chemical reactions for the synthesis of nitrogen-containing chemicals. This class of substances are vital for human health since they are commonly found in pharmaceuticals. Despite the advancements made in medical science over the past several decades, there is still a lack of effective treatment for many diseases. To meet the pressing demand for new cures, more facile syntheses of biologically active compounds are required. To this end, this project aimed to streamline the synthesis of nitrogen-containing molecules through the development of novel chemical reactions.

Work performed from the beginning of the project to the end of the period covered by the report and main results achieved so far

A novel chemical reaction for the modification of proteins and peptides, a class of nitrogen-containing compounds, is developed. The reaction makes a structural change to existing proteins or peptides and thus provides a method for obtaining novel biologically active compounds. While proteins and peptides are highly complex compounds, the reaction is highly selective for a specific part of their structure, affording well-defined products. The mild reaction conditions used are also an important feature because proteins and peptides are prone to decomposition. Publication in a high impact journal is expected to publicize this novel reaction, allowing its application in both academia and industry.

Progress beyond the state of the art and expected potential impact (including the socio-economic impact and the wider societal implications of the project so far)

Despite many existing protocols for protein and peptide modification, the reaction developed selectively transforms proteins and peptides in a way that cannot be currently achieved. Therefore, it is expected to find applications in biochemistry and medicinal chemistry. For instance, it may be applied to probe how a protein or peptide carries out its functions in the human body. Such investigations will be important for understanding the cause of certain diseases and for enabling the development of new cures. In addition, the reaction developed can be applied to transform proteins or peptides which are currently used as drugs. The change in structure induced by this reaction could lead to an improvement in pharmacological properties, such as increased potency and reduced side effects. In summary, the outcome of the project could have broad implications in the forefront of biological and medical research.

Protein and Peptide Modification