16163-78-3Relevant academic research and scientific papers
N-substituted (2,3-dihydro-1,4-benzodioxin-2-yl)methylamine derivatives as 92 antagonists/5-HT(1A) partial agonists with potential as atypical antipsychotic agents
Birch, Alan M.,Bradley, Paul A.,Gill, Julie C.,Kerrigan, Frank,Needham, Pat L.
, p. 3342 - 3355 (2007/10/03)
A series of N-substituted 1-(2,3-dihydro-1,4-benzodioxin-2- yl)methylamine derivatives with D2 antagonist/5-HT(1A) partial agonist activity has been prepared as potential atypical antipsychotic agents. Optimization of in vitro receptor binding activity and in vivo activity in rodent models of psychosis has led to compound 24, which showed good affinities for human D2, D3, and 5-HT(1A) receptors but significantly less affinity for human α1 adrenoceptors and rat H1 and muscarinic receptors. In rodents, 24 showed functional D2-like antagonism and 5-HT(1A) partial agonism. After oral dosing, 24 showed good activity in rodent antipsychotic tests and very little potential to cause extrapyramidal side effects (EPS), as measured by its ability to induce catalepsy in rats only at very high doses. In the light of this promising profile of activity, 24 has been selected for clinical investigation as a novel antipsychotic agent with a predicted low propensity to cause EPS.
On the Reaction of α-(2-Hydroxyphenoxy)alkylketones with Dimethylsulphoxonium Methylide. A Novel Route to 2-Substituted-2,3-dihydro-2-hydroxymethyl-1,4-benzodioxins
Salimbeni, Aldo,Manghisi, Elso,Arnone, Alberto
, p. 943 - 947 (2007/10/02)
A new route to 2-substituted-2,3-dihydro-2-hydroxymethyl-1,4-benzodioxins 3 based on the reaction of α-(2-hydroxyphenoxy)alkylketones 1 with dimethylsulphoxonium methylide in dimethylsulphoxide is reported.Besides the desired compounds 3, the isomeric 2H-
