69478-77-9Relevant articles and documents
Chiral 3-aminopyrrolidines as a rigid diamino scaffold for organocatalysis and organometallic chemistry
Pouliquen, Mickael,Blanchet, Jerome,Paolis, Michael De,Rema Devi,Rouden, Jacques,Lasne, Marie-Claire,Maddaluno, Jacques
experimental part, p. 1511 - 1521 (2010/11/02)
Over 20 new and easily prepared diamines were screened for the asymmetric Morita-Baylis-Hillman reaction. Chiral non-racemic 3-(N,N-dimethylamino)-1- methylpyrrolidine was found to promote efficiently the reaction of methyl vinyl ketone and substituted benzaldehydes. Enantiomeric excesses up to 73% were reached with electron-deficient benzaldehyde derivatives. After a simple deprotonation, one of these diamines was transformed into a chiral mixed aggregate for the enantioselective synthesis of (R)-1-o-tolylethanol with 76% ee.
Dibenzo-epines: Effect of the basic side-chain on neuroleptic activity
Burki,Fischer,Hunziker,et al.
, p. 479 - 485 (2007/10/05)
Structure-activity relationships in a series of dibenzo[b,f][1,4]thiazepines and -oxazepines and dibenzo[b,e][1,4]diazepines having different basic substituents in the 11-position were studied with reference to their neuroleptic activity. A high degree of structure-specificity was found for the piperazinyl moiety as well as for the distances between the distal nitrogen atom of this group and the tricyclic ring system, which distances are probably of importance for receptor binding. It was shown that the N-oxides of the neuroleptic agents clotiapine, loxapine and clozapine were inactive in in vitro binding tests involving central dopaminergic receptors, and it is very likely therefore that the in vivo activity of these N-oxides in the rat is due to their enzymatic reduction to the active parent compounds. All derivatives having a basic side-chain other than N-alkylpiperazinyl were inactive neuroleptically, with the exception of the N-methyl-4-piperidyl derivative which showed relatively weak effects.
