202828-84-0Relevant articles and documents
Preparation of monoalkylpiperidines via the mild hydrogenation of monoalkynylpyridines
Usuki, Toyonobu,Komatsu, Akira
, p. 2856 - 2858 (2017)
Monoalkynylpyridines were prepared via a Sonogashira cross-coupling reaction between monoiodopyridines and alkynes. Mild hydrogenation of the obtained monoalkynylpyridines was then conducted to produce the corresponding monoalkylpiperidines in moderate to excellent yields. The hydrogenation reaction was carried out under H2 (1?atm) in the presence of 10?wt% Pd/C (5?eq) in either AcOH or MeOH at room temperature. The present mild method is therefore useful for the quick and easy preparation of monoalkylpiperidines.
An Orally Bioavailable, Indole-3-glyoxylamide Based Series of Tubulin Polymerization Inhibitors Showing Tumor Growth Inhibition in a Mouse Xenograft Model of Head and Neck Cancer
Colley, Helen E.,Muthana, Munitta,Danson, Sarah J.,Jackson, Lucinda V.,Brett, Matthew L.,Harrison, Joanne,Coole, Sean F.,Mason, Daniel P.,Jennings, Luke R.,Wong, Melanie,Tulasi, Vamshi,Norman, Dennis,Lockey, Peter M.,Williams, Lynne,Dossetter, Alexander G.,Griffen, Edward J.,Thompson, Mark J.
, p. 9309 - 9333 (2015/12/23)
A number of indole-3-glyoxylamides have previously been reported as tubulin polymerization inhibitors, although none has yet been successfully developed clinically. We report here a new series of related compounds, modified according to a strategy of redu
Rhodium(III)-catalyzed isoquinolone synthesis: The N-O bond as a handle for C-N bond formation and catalyst turnover
Guimond, Nicolas,Gouliaras, Christina,Fagnou, Keith
supporting information; experimental part, p. 6908 - 6909 (2010/07/05)
An external-oxidant-free process to access the isoquinolone motif via cross-coupling/cyclization of benzhydroxamic acid with alkynes is described. The reaction features a regioselective cleavage of a C-H bond on the benzhydroxamic acid coupling partner as well as a regioselective alkyne insertion. Mechanistic studies point out the important involvement of a N-O bond as a tool for C-N bond formation and catalyst turnover.