The application of flow microreactors to the preparation of a family of casein kinase I inhibitors

Graphical Abstract

The Application of Flow Microreactors to the Preparation of a Family of Casein Kinase I Inhibitors.
Venturoni, F.; Nikbin, N.; Ley S. V.; Baxendale, I. R.
Org. Biomol. Chem. 2010, 8, 1798-1806. Link: 10.1039/b925327k http://pubs.rsc.org/en/Content/ArticleLanding/2010/OB/b925327k#!divAbstract

In this article we demonstrate how a combination of enabling technologies such as flow synthesis, solid-supported reagents and scavenging resins utilised under fully automated software control can assist in typical medicinal chemistry programmes. In particular automated continuous flow methods have greatly assisted in the optimisation of reaction conditions and facilitated scale up operations involving hazardous chemical materials. Overall a collection of twenty diverse analogues of a casein kinase I inhibitor has been synthesised by changing three principle binding vectors.

Francesco Venturoni,^a Nikzad Nikbin,^a Steven V. Ley^a and Ian R. Baxendale^a

^aInnovative Technology Centre, Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge, UK

E-mail: TheITC@ch.cam.ac.uk

Org. Biomol. Chem., 2010,8, 1798-1806

DOI: 10.1039/B925327K