21903-93-5Relevant academic research and scientific papers
SUBSTITUTED HETEROARYL COMPOUNDS AND METHODS OF USE THEREOF
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, (2015/02/25)
Provided herein are novel heteroaryl compounds, pharmaceutically acceptable salts and pharmaceutical formulations thereof for selectively inhibiting serotonin reuptake and/or acting as 5-HT1A receptor agonists. Also provided herein are pharmaceutical compositions comprising the heteroaryl compounds and methods of using the pharmaceutical compositions in treating central nervous system (CNS) dysfunction in a mammal, especially a human being.
SUBSTITUTED PIPERAZINE COMPOUNDS AND METHODS AND USE THEREOF
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Paragraph 00227; 00316, (2015/11/27)
Provided herein are novel piperazine compounds acting as selective serotonin reuptake inhibitors and/or the 5-HT1A receptor agonists. The invention also relates to the methods of preparing the compound and pharmaceutical composition, and the use of treating central nervous system dysfunction in mammals especially in humans.
Synthesis of 1-substituted 4-[4-(1H-indol-3-yl)butyl]piperazines
Labanauskas, Linas,Mazeikaite, Rita,Urbelis, Gintaras,Gedrimaite, Olga,Sudzius, Jurgis,Cikotiene, Inga
, p. 363 - 376 (2014/01/23)
A convenient synthetic route for preparation of various 4-[4-(1H-indol-3-yl)butyl]piperazines bearing heterocyclic and aliphatic substituents in position 1 has been developed. During this work some synthetic possibilities of common precursor, 4-[4-(1H-indol-3-yl)butyl]piperazine, were studied and evaluated. ARKAT-USA, Inc.
Electrophilic Substitution in Indoles. Part 13. The Synthesis and Rearrangement of 2-Deuteriospiro
Ibaceta-Lizana, Juana S. L.,Jackson, Anthony H.,Prasitpan, Noojare,Shannon, Patrick V. R.
, p. 1221 - 1226 (2007/10/02)
2-Deuterioindole was prepared from N-phenylsulphonylindole by lithiation, quenching with D2O, and hydrolysis.Treatment of the 2-deuterioindole Grignard reagent with succinic anhydride gave 4-(indol-3-yl)-4-oxobutanoic acid with partial loss of the deuterium from the 2-position. 2,3-Dideuterioindole (prepared by acid-catalysed deuteration of 2-deuterioindole) when treated in the same way, gave the indolyl oxobutanoic acid, 92 percent deuteriated at the indolyl 2-position.Reduction to the deuterioindolylbutanol and treatment of its toluene-p-sulphonate with potassium t-butoxide give 2-deuterio-spiro which was 88 percent deuteriated at the 2-position.The kinetics of the acid-catalysed rearrangement of the deuterioindolenine and its non-deuteriated analogue were measured and the ratio kH/kD of the pseudo-first-order rate constants was found to be 1.08, showing that the isotope effect was very small.
