290366-76-6Relevant academic research and scientific papers
Asymmetric synthesis of piperidines using the nitro-Mannich reaction☆
Anderson, James C.,Bouvier-Israel, Eva,Rundell, Christopher D.,Zhang, Xiangyu
, (2020/12/21)
A method for the synthesis of functionalized piperidines containing 3 contiguous stereocentres in the 2-,3- and 4- positions uses a diastereoselective nitro-Mannich to control stereochemistry. The nitro-Mannich reaction between a β-aryl/heteroaryl substituted nitroalkanes and glyoxylate imine provides β-nitro-amines with good selectivity (70:30 to >95:5) for the syn, anti-diastereoisomers. Reductive cyclisation with BF3.OEt2 and Et3SiH gave, after purification, stereochemically pure piperidines in 19–57% yield for ten examples with different 4-aryl/heteroaryl substituents.
Potent and selective α1A adrenoceptor partial agonists-Novel imidazole frameworks
Whitlock, Gavin A.,Brennan, Paul E.,Roberts, Lee R.,Stobie, Alan
scheme or table, p. 3118 - 3121 (2010/01/16)
Novel imidazole frameworks have been identified as potent partial agonists of the α1A adrenergic receptor, with good selectivity over the α1B, α1D and α2A receptor sub-types. Nitrile 28 possessed attractive CNS
