126640-10-6Relevant articles and documents
Haloperidol metabolite II prodrug: Asymmetric synthesis and biological evaluation on rat C6 glioma cells
Sozio, Piera,Fiorito, Jole,Di Giacomo, Viviana,Di Stefano, Antonio,Marinelli, Lisa,Cacciatore, Ivana,Cataldi, Amelia,Pacella, Stephanie,Turkez, Hasan,Parenti, Carmela,Rescifina, Antonio,Marrazzo, Agostino
, p. 1 - 9 (2015)
In a previous work we reported the antiproliferative effects of (±)-MRJF4, a novel haloperidol metabolite II (HP-mII) (a sigma-1 antagonist and sigma-2 agonist) prodrug, obtained through conjugation to 4-phenylbutyric acid (PhBA) [a histone deacetylase in
Chemoenzymatic synthesis of (R)-(+)-α-(4-fluorophenyl)-4-(2-pyrimidinyl)-1-piperazinebutanol and (R)-(+)-α-(4-fluorophenyl)-4-methyl-1-piperidinebutanol as potential antipsychotic agents
Gil, Nicolas,Bosch, Ma. Pilar,Guerrero, Angel
, p. 15115 - 15122 (1997)
A chemoenzymatic straightforward synthesis of (R)-(+)-α-(4-fluorophenyl)-4-methyl-1-piperidinebutanol (2) and (R)-(+)-α-(4-fluorophenyl)-4-(2-pyrimidinyl)-1-piperazinebutanol (3), two potential antipsychotic agents, has been developed by two different approaches involving lipase-mediated resolution of the racemic compounds or through asymmetrization of the precursor alcohol 4. A second enzymatic resolution followed by condensation of (R)-4 with 4-methylpiperidine (6) or 1-(2-pyrimidinyl)piperazine (7) leads to (R)-2 and (R)-3 in good chemical and excellent optical yields (>99% ee).
A convenient enantioselective CBS-reduction of arylketones in flow-microreactor systems
De Angelis, Sonia,De Renzo, Maddalena,Carlucci, Claudia,Degennaro, Leonardo,Luisi, Renzo
supporting information, p. 4304 - 4311 (2016/05/24)
A convenient, versatile, and green CBS-asymmetric reduction of aryl and heteroaryl ketones has been developed by using the microreactor technology. The study demonstrates that it is possible to handle borane solution safely within microreactors and that the reaction performs well using 2-MeTHF as a greener solvent.
