- Imidazo[1,2- a]pyridine derivatives as aldehyde dehydrogenase inhibitors: Novel chemotypes to target glioblastoma stem cells
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Glioblastoma multiforme (GBM) is the deadliest form of brain tumor. It is known for its ability to escape the therapeutic options available to date thanks to the presence of a subset of cells endowed with stem-like properties and ability to resist to cyto
- Quattrini, Luca,Gelardi, Edoardo Luigi Maria,Coviello, Vito,Sartini, Stefania,Ferraris, Davide Maria,Mori, Mattia,Nakano, Ichiro,Garavaglia, Silvia,La Motta, Concettina
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p. 4603 - 4616
(2020/06/08)
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- Oxidative Cross-Coupling of sp3- and sp2-Hybridized C-H Bonds: Vanadium-Catalyzed Aminomethylation of Imidazo[1,2-a]pyridines
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The vanadium-catalyzed oxidative coupling of substituted 2-arylimidiazo[1,2-a]pyridines to N-methylmorpholine oxide, which acts as both a coupling partner and an oxidant, has been achieved. This reaction was applied to various substituted imidiazo[1,2-a]pyridine and indole substrates, resulting in yields as high as 90%. Mechanistic investigations indicate that the reaction may proceed via a Mannich-type process. This work demonstrates how oxidative aminomethylation can be used as a useful method to introduce tertiary amines into heterocycles, thus providing an alternative method for conventional Mannich-type reactions.
- Kaswan, Pinku,Porter, Ashley,Pericherla, Kasiviswanadharaju,Simone, Marissa,Peters, Sean,Kumar, Anil,Deboef, Brenton
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supporting information
p. 5208 - 5211
(2015/11/18)
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