| Title : Synthesis of two fluoro analogues of the nicotinic acetylcholine receptor agonist UB-165 - Sutherland_2003_J.Org.Chem_68_2475 |
| Author(s) : Sutherland A , Gallagher T , Sharples CG , Wonnacott S |
| Ref : J Org Chem , 68 :2475 , 2003 |
|
Abstract :
Two racemic fluoropyridine analogues 4 and 5 of the potent nicotinic agonist UB-165 have been synthesized. Halogenated pyridines 7 and 12 provided the organometallic reagents needed for the Negishi and Suzuki coupling reactions used for the preparation of 4 and 5, and the N-vinyloxycarbonyl protecting group of 8 and 15 was cleaved using a novel trifluoroacetic acid-mediated deprotection protocol. Analogue 4 retained high binding affinity at rat brain alpha4beta2 and alpha7 nicotinic receptors. |
| PubMedSearch : Sutherland_2003_J.Org.Chem_68_2475 |
| PubMedID: 12636420 |
Sutherland A, Gallagher T, Sharples CG, Wonnacott S (2003)
Synthesis of two fluoro analogues of the nicotinic acetylcholine receptor agonist UB-165
J Org Chem
68 :2475
Sutherland A, Gallagher T, Sharples CG, Wonnacott S (2003)
J Org Chem
68 :2475