3289-98-3Relevant academic research and scientific papers
Chiral γ - amino alcohol compound preparation method
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Paragraph 0039-0040, (2018/11/26)
The invention discloses a preparation method of a chiral gamma-aminoalcohol compound. In the condition of a certain hydrogen pressure and a temperature, with the effects of solvents and a alkali, a ruthenium chiral catalyst is used for catalyzing a beta-amino ketone compound (I) for generating an asymmetric catalytic hydrogenation reaction, and the chiral gamma-aminoalcohol compound (II) is prepared. The preparation method of the present invention has the advantages of mild condition, low cost, few environment influences, good reaction yield, enantioselectivity and good application prospect.
SUBSTITUTED 3-HETEROARYLOXY-3-(HETERO)ARYL-PROPYLAMINES AS SEROTONIN TRANSPORTER AND SEROTONIN HT2C RECEPTOR MODULATORS
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Page/Page column 12-13; 23, (2014/04/04)
The present invention relates to compounds compound according to Formula (1): and pharmaceutically acceptable salts, hydrates and solvates thereof. These compounds have serotonin (5-HT) transporter inhibitory effects and 5-HT 2C receptor antagonist or inverse agonist effects. The present invention also relates to pharmaceutical compositions comprising these compounds, and methods of using them for application in the prophylaxis or treatment of CNS disorders.
Synthesis and preliminary biological characterization of a new potential 125I-radioligand for dopamine and serotonin receptors
Guarna,Menchi,Berti,Cini,Bottoncetti,Raspanti,Politi,Pupi
, p. 3197 - 3206 (2007/10/03)
The synthesis and a preliminary biological characterization of a new class of N-benzyl-aminoalcohols which have serotonin (5-HT2) and dopamine (D2) receptor affinity is described. In vitro competition binding studies were conducted with the new molecules and 3H-spiperone on crude membrane preparation from rat striatum and frontal cortex. One of these compounds, 3-benzylamino-1-(4-fluoro-2-iodophenyl)-propan-1-ol (6f), whose IC50 values are in the micromolar range for both the D2 and 5-HT2 receptors, was prepared in iodine-125 labelled form (6i) by nucleophilic substitution of the bromine atom of 3-benzylamino-1-(2-bromo-4-fluorophenyl)-propan-1-ol (6d). In the in vivo studies, conducted on rats, the radiolabelled molecule 6i shows a good capacity to cross the blood-brain barrier (BBB) with a mean value of first pass cerebral extraction (E) of ca. 50% when the regional cerebral blood flow, measured with microsphere technique, is in the experimental animal's physiologic range (0.8-1 mL/min/g). A preliminary in vitro autoradiographic distribution on coronal rat brain slices of the radioiodinated molecule showed that it was preferentially localized in the striatum and in the cerebral regions rich in dopamine- and serotonin receptors, even if a high non-specific binding was observed.
