16531-06-9Relevant academic research and scientific papers
Iridium-Catalyzed Aza-Spirocyclization of Indole-Tethered Amides: An Interrupted Pictet-Spengler Reaction
Gabriel, Pablo,Gregory, Alex W.,Dixon, Darren J.
supporting information, p. 6658 - 6662 (2019/08/30)
A mild, reductive spirocyclization of indole-linked amides and lactams for the efficient and selective synthesis of aza-spirocyclic indoline products is described. The catalytic reductive activation of tertiary amides or lactams by Vaska's complex with tetramethyldisiloxane as the terminal reductant allowed iminium ion formation, before a diastereoselective 5-endo-trig spirocyclization of the tethered indole moiety was triggered. Terminal reduction affords the aza-spiroindoline products in an overall highly chemoselective and diastereoselective one-pot process.
Design, synthesis and biological activity of new CDK4-specific inhibitors, based on fascaplysin
Aubry, Carine,Wilson, A. James,Jenkins, Paul R.,Mahale, Sachin,Chaudhuri, Bhabatosh,Marechal, Jean-Didier,Sutcliffe, Michael J.
, p. 787 - 801 (2007/10/03)
We present the design, synthesis, and biological activity of three classes of tryptamine derivatives, which are non-planar analogues of the toxic anti-cancer agent fascaplysin. We show these compounds to be selective inhibitors of CDK4 over CDK2, the most active compound 9q has an IC50 for the inhibition of CDK4 of 6 M. The Royal Society of Chemistry 2006.
