454422-74-3Relevant academic research and scientific papers
Chiral drugs via the spontaneous resolution
Kostyanovsky, Remir G.,Kadorkina, Gul'nara K.,Lyssenko, Konstantin A.,Torbeev, Vladimir Yu.,Kravchenko, Angelina N.,Lebedev, Oleg V.,Grintselev-Knyazev, Gennadii V.,Kostyanovsky, Vasily R.
, p. 6 - 8 (2002)
The psychotropically active drug Albicar 1 has been prepared for the first time in both enantiomerically pure forms starting from the (+)-2 and (-)-2 precursors obtained by spontaneous resolution; the crystal structures of (-)-1 and (±)-1 have been solved by X-ray diffraction study.
Preparative synthesis and pharmacological activity of Albicar racemate and enantiomers
Anikina, Lada V.,Vikharev, Yuri B.,Baranov, Vladimir V.,Malyshev, Oleg R.,Kravchenko, Angelina N.
, p. 317 - 319 (2018/06/01)
Racemic Albicar (2,6-diethyl-4,8-dimethylglycoluril) has been synthesized and resolved into enantiomers on a preparative scale by chiral HPLC. A comparison of the pharmacological effects of these compounds has been performed for the first time. It has been demonstrated that the (?)-(1S,5S)-enantiomer exerts a stimulating effect on the central nervous system due to activation of the serotonergic system, since it potentiates the effects of 5-hydroxytryptophan (the serotonin precursor), while the antagonist of serotonin receptors blocks its activity; the (+)-(1R,5R)-enantiomer evinces an inhibitory effect.
The chiral drug Albicar: Resolution of its racemate via complexation with BINOL
Lenev, Denis A.,Lyssenko, Konstantin A.,Kostyanovsky, Remir G.
experimental part, p. 403 - 404 (2010/06/14)
Both enantiomers of the title drug (2,6-diethyl-4,8-dimethyl-glycoluril; 1) were prepared from their complexes with (R)- and (S)-BINOL in 59% ((+)-1) and 43% ((-)-1) yield from its racemate. The absolute configuration of (1R,5R)-(+)-1 was determined by an
