- Diastereoselective synthesis of 4-hydroxypiperidin-2-ones via Cu(I)-catalyzed reductive aldol cyclization
-
(Chemical Equation Presented) 4-Hydroxypiperidin-2-ones may be prepared in highly diastereoselective fashion using a Cu(I)-catalyzed reductive aldol cyclization of αβ-unsaturated amides with ketones. Used in combination with proline-catalyzed asymmetric M
- Hon, Wai Lam,Murray, Gordon J.,Firth, James D.
-
p. 5743 - 5746
(2007/10/03)
-
- Opioid properties of some isomeric derivatives of phencyclidine
-
The phencyclidine analogues (±)-α-, (±)-β-, and (+)-α- and (-)-α-4-hydroxy-3-methyl-4-phenyl-1-(1-phenylcyclohexyl) piperidene, all with known relative and absolute stereochemistry, have been prepared, and their analgesic potencies related to correspondin
- Casy,Dewar,Al-Deeb
-
-
- Combined analgesic/neuroleptic activity in N-butylrophenone prodine-like compounds
-
Some 4-phenyl-4-piperidinols, corresponding esters, and related compounds with a p-fluorobutyrophenone chain on nitrogen were synthesized and evaluated in in vitro and in vivo tests in order to examined their ability to interact contemporaneously with opioid and dopamine receptors. The propionyloxy derivatives showed a good combination of analgesic and neuroleptic activity. With a 3-methyl substituent on the piperidine ring, the β-configuration was the more active form not only for analgesic activity, as expected from previous results on prodines, but also for neuroleptic activity. Haloperidol and its propionate were also tested as reference compounds.
- Iorio,Raymer,Frigeni
-
p. 1906 - 1910
(2007/10/02)
-