46817-91-8Relevant articles and documents
Lewis acid mediated intramolecular C-O bond formation of alkanol-epoxide leading to substituted morpholine and 1,4-oxazepane derivatives: Total synthesis of (±)-Viloxazine
Ghosh, Priya,Deka, Manash J.,Saikia, Anil K.
, p. 690 - 698 (2016/01/15)
Substituted morpholines have been efficiently synthesised in good yields from nitrogen tethered alkanol-epoxide mediated by boron trifluoride etherate. The methodology has been used for the total synthesis of (±)-viloxazine.
METHODS FOR PRODUCING VILOXAZINE SALTS AND NOVEL POLYMORPHS THEREOF
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, (2011/10/19)
Provided here are methods of manufacture of viloxazine and its various salts, as well as viloxazine-related compounds, such as novel intermediate reaction products and polymorphs thereof. In particular, the methods provide a substantially pure API of viloxazine HCl while avoiding undesirable impurities. The methods further provide for separating, identifying, and characterizing novel polymorphs of viloxazine. Further provided are methods for synthesis and identification and characterization of novel intermediates of viloxazine, as well as for some important metabolites and precursors of metabolites of viloxazine.
2-Aryloxymethylmorpholine histamine H3 antagonists
Letavic, Michael A.,Keith, John M.,Ly, Kiev S.,Bonaventure, Pascal,Feinstein, Mark A.,Lord, Brian,Miller, Kirsten L.,Motley, S. Timothy,Nepomuceno, Diane,Sutton, Steven W.,Carruthers, Nicholas I.
scheme or table, p. 5796 - 5799 (2009/11/30)
The synthesis and biological activity of a new series of 2-aryloxymethylmorpholine histamine H3 antagonists is described. The new compounds are high affinity histamine H3 ligands that penetrate the CNS and occupy the histamine H3 receptor in rat brain.
New series of morpholine and 1,4-oxazepane derivatives as dopamine D 4 receptor ligands: Synthesis and 3D-QSAR model
Audouze, Karine,Nielsen, Elsebet ?stergaard.,Peters, Dan
, p. 3089 - 3104 (2007/10/03)
Since the identification of the dopamine D43 receptor subtype and speculations about its possible involvement in schizophrenia, much work has been put into development of selective D4 ligands. These selective ligands may be effective antipsychotics without extrapyramidal side effects. This work describes the synthesis of a new series of 2,4-disubstituted morpholines and 2,4-disubstituted 1,4-oxazepanes with selectivity for the dopamine D4 receptor. A 3D-QSAR analysis using the GRID/GOLPE methodology was performed with the purpose to get a better understanding of the relationship between chemical structure and biological activity. Inspection of the coefficient plots allowed us to identify that regions which are important for affinity are situated around the two benzene ring systems, a p-chlorobenzyl group, and the aliphatic amine belonging to the morpholine or 1,4-oxazepane system. In addition, the size of the morpholine or 1,4-oxazepane ring seems to be important for affinity.
2 Aryloxymethyl 2,3,5,6 tetrahydro 1,4 oxazines, a new class of antidepressants
Greenwood,Mallion,Todd,Turner
, p. 573 - 577 (2007/10/05)
Some 2 aryloxymethyl 2,3,5,6 tetrahydro 1,4 oxazines have been shown to possess marked antidepressant activity. The 1,4 oxazines were synthesized by lithium aluminium hydride reduction of the readily available 6 aryloxymethyl 2,3,5,6 tetrahydro 1,4 oxazin 3 ones. High antidepressant activity was associated with ortho substitution of the 2 phenoxymethyl group and with 1,4 oxazines devoid of 4 substituents.
