The application of flow microreactors to the preparation of a family of casein kinase I inhibitors.
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.
Venturoni
Francesco
F
Innovative Technology Centre, Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge, UKCB2 1EW.
Nikbin
Nikzad
N
Ley
Steven V
SV
Baxendale
Ian R
IR
D047389:Casein Kinase I / Q000037:antagonists & inhibitors*; D020650:Combinatorial Chemistry Techniques / Q000295:instrumentation* / Q000379:methods; D004867:Equipment Design; D015394:Molecular Structure; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry; D011724:Pyridazines / Q000138:chemical synthesis* / Q000737:chemistry
D047428:Protein Kinase Inhibitors; D011724:Pyridazines; D047389:Casein Kinase I