57691-97-1Relevant academic research and scientific papers
N-Heterocyclic Carbene-Mediated Microfluidic Oxidative Electrosynthesis of Amides from Aldehydes
Green, Robert A.,Pletcher, Derek,Leach, Stuart G.,Brown, Richard C. D.
supporting information, p. 1198 - 1201 (2016/03/15)
A flow process for N-Heterocyclic Carbene (NHC)-mediated anodic oxidative amidation of aldehydes is described, employing an undivided microfluidic electrolysis cell to oxidize Breslow intermediates. After electrochemical oxidation, the reaction of the intermediate N-acylated thiazolium cation with primary amines is completed by passage through a heating cell to achieve high conversion in a single pass. The flow mixing regimen circumvented the issue of competing imine formation between the aldehyde and amine substrates, which otherwise prevented formation of the desired product. High yields (71-99%), productivities (up to 2.6 g h-1), and current efficiencies (65-91%) were realized for 19 amides.
Design, synthesis and biological evaluation of new tryptamine and tetrahydro-β-carboline-based selective inhibitors of CDK4
Jenkins, Paul R.,Wilson, James,Emmerson, Daniel,Garcia, Marcos D.,Smith, Matthew R.,Gray, Stephen J.,Britton, Robert G.,Mahale, Sachin,Chaudhuri, Bhabatosh
, p. 7728 - 7739 (2008/12/23)
We present the design, synthesis and biological activity of a library of substituted (biphenylcarbonyl)-tryptamine and (biphenylcarbonyl)-tetrahydro-β-carboline compounds related to the natural product fascaplysin, as novel inhibitors of CDK4/cyclin D1. We show all these molecules, prepared using the Suzuki-Miyaura reaction, being selective inhibitors of CDK4 over CDK2. The most active compounds have a CDK4 IC50 in the range 9-11 μM, three of them containing the para-biphenyl plus para-substituents supporting the existence of a π-stacking pocket within the active site of CDK4.
