First total synthesis of (+/-)-3-hydroxy-11-norcytisine: structure confirmation and biological characterization
Daniel Yohannes1, Camilla P Hansen, Srinivasa Rao Akireddy
1Targacept, Inc., 200 East First Street, Suite 300, Winston-Salem, North Carolina 27101, USA. daniel.yohannes@targacept.com
Abstract:
The first total synthesis of the natural product 3-hydroxy-11-norcytisine (1), structurally related to cytisine (2), a benchmark ligand at neuronal nicotinic acetylcholine receptors (NNRs), has been achieved. The synthesis permits the unambiguous confirmation of the structure originally proposed for 1 and has enabled initial biological characterization of 1 and its related compounds against NNRs.
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