Development of new protocols for the synthesis of arrays of heterocycles
Lead Research Organisation:
University of Nottingham
Department Name: Sch of Chemistry
Abstract
Heterocyclic compounds, cyclic molecules in which one or more carbon atom is replaced by a heteroatom (commonly nitrogen, oxygen or sulfur) account for well over half of all known organic compounds. Many classes of natural products, as well as a large majority of commercially important drugs, agrochemicals, reprographic materials, dyes, etc., contain heterocyclic rings. Hence the synthesis and study of heterocyclic compounds, in particular nitrogen containing rings, is a subject of immense importance both for academia and industry. The commercial relevance of heterocyclic compounds is amply demonstrated by the list of best selling pharmaceuticals. In the 12 months to June 2005, seven of the top ten best sellers were nitrogen heterocycles with combined sales of $41 billion (out of $55.7 billion for the top ten). This proposal, which has the full support of GSK, seeks support to develop some new methods for the efficient and rapid laboratory preparation of arrays of heterocyclic molecules as potential medicines. Arrays are sets of compounds, usually prepared simultaneously by automated methods, where structural components of the molecule are varied systematically. Although array synthesis is a fundamental tool in modern medicinal chemistry, the reactions that can be used remain somewhat limited, and therefore new methods and protocols are urgently sought.
People |
ORCID iD |
Christopher Moody (Principal Investigator) |
Publications
Shi B
(2009)
The rhodium carbene route to oxazoles: a remarkable catalyst effect.
in Chemical communications (Cambridge, England)
Shi B
(2010)
Rhodium carbene routes to oxazoles and thiazoles. Catalyst effects in the synthesis of oxazole and thiazole carboxylates, phosphonates, and sulfones.
in The Journal of organic chemistry
Shi B
(2009)
A concise route to pyridines from hydrazides by metal carbene N-H insertion, 1,2,4-triazine formation, and Diels-Alder reaction.
in Organic letters
Honey M
(2014)
Synthesis of Indoxylic Acid Esters by Rhodium-catalyzed Carbene N-H Insertion and Thermal Cyclization
in Australian Journal of Chemistry
Description | In subsequent grant applications, publications and conference presentations |
First Year Of Impact | 2008 |
Sector | Chemicals,Healthcare,Pharmaceuticals and Medical Biotechnology |
Impact Types | Economic |
Description | EPSRC |
Amount | £253,824 (GBP) |
Funding ID | EP/G027919/1 |
Organisation | Engineering and Physical Sciences Research Council (EPSRC) |
Sector | Public |
Country | United Kingdom |
Start | 10/2009 |
End | 09/2012 |