33130-23-3Relevant academic research and scientific papers
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.
Self-activated supramolecular reactions: Effects of host-guest recognition on the kinetics of the Diels-Alder reaction of open-chain oligoether quinones with cyclopentadiene
Tsuda, Akihiko,Fukumoto, Chikako,Oshima, Takumi
, p. 5811 - 5822 (2007/10/03)
Diels-Alder reactions of acyclic oligoether-substituted quinones 1b, 1c, 2b, and 2c with cyclopentadiene were accelerated by the addition of alkali and alkaline earth metal perchlorates, and scandium trifluoromethane sulfonate (kc/kf
Disubstituted morpholine, oxazepine or thiazepine derivatives, their preparation and their use as dopamine D4 receptor antagonists
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, (2008/06/13)
The present invention relates to compounds of formula (I), any of it enantiomers, or any mixture thereof, or a pharmaceutically acceptable acid addition salt thereof, wherein R1, R2, R3, R4, R11, R12, R13, R14and R15each independently are hydrogen, alkyl, alkoxy, halogen, trifluoromethyl, nitro, cyano, amino, acyl, alkylamino, dialkylamino, aminocarbonyl, or acylamino; R5 is hydrogen, alkyl, alkoxyalkyl, or phenylalkyl; X is —CH2—Z—, Z—CH2—, NH—CO—, —CO—NH—, or —CH═CH—; wherein Z is O, S, CH2, or NH; Y is O, —CH2—W—, —W—CH2—; wherein W is O, or S; and n is 0, 1 or 2. The compounds are useful in the treatment of psychotic disorders.
Reactions of Co-ordinated Ligands. Part 8. Reaction of Grignard Reagents with 2-Alkoxy-1,3-dioxolans; an Improved Route to Aldehydes
Houghton, Roy P.,Morgan, Alan D.
, p. 756 - 758 (2007/10/02)
The yields of 2-phenyl-1,3-dioxolan obtained from phenylmagnesium bromide and 2-alkoxy-1,3-dioxolans in which the type Men-O increase as the value of n proceeds along the series 4,3,1,2.Several Grignard reagents(including phenylmagnesium bromide) react with the 2-alkoxy-1,3-dioxolan in which n=2 to give the expected 2-substituted-1,3-dioxolans, whose yields are considerably higher than those of the diethyl acetals obtained from the corresponding reation with ethyl ortoformate.
