Applications of Multicomponent Reactions in Drug Discovery - Lead Generation to Process Development

Applications of Multicomponent Reactions in Drug Discovery - Lead Generation to Process Development 

The advantage of an MCR synthesis over an equivalent linear synthesis is clear, in that the size of a linear derived library is a function of the number of steps and individual inputs. For example, the library from a three-step synthesis with 10 inputs at each step would have a size of 103 compounds, whereas that from a three- 

Multicomponent Reactions. Edited by Jieping Zhu, Hugues Bienayme Copyright 2005 WILEY-VCH Veriag GmbH Co. KGaA, Weinheim ISBN 3-527-30806-7 

So what value do MCR methodologies bring to the discovery table The following come quickly to mind in chronological order from early to late stage discovery  

Scaffold development cycles (often cited at six months per core for a 4-5-step linear solid phase route) are dramatically shortened. Eight novel production-ready cores were constructed by one full-time equivalent over a 12-month period in this laboratory. 

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Hulme C (2005) Applications of multicomponent reactions in drug discovery - lead generation to process development. In Zhu J, Bienayme H (eds) Multicomponent reactions. Wiley-VCH, Weinheim, pp 311-341... 

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