56660-98-1

Upstream product

• 19668-18-9 1-<4-(4-fluorophenyl)-4,4-(ethylenedioxy)butyl>-4-hydroxypiperidine 
• 41979-39-9 4-piperidone hydrochloride 
• 3308-94-9 4-chloro-1-(4-fluorophenyl)-1,1-(ethylenedioxy)butane 
• 40064-34-4 piperidine-4,4-diol hydrochloride 

Downstream Products

• 1026686-74-7 1-{3-[2-(4-fluoro-phenyl)-[1,3]dioxolan-2-yl]-propyl}-4-methylamino-piperidine-4-carbonitrile 
• 1026321-49-2 4-cyclohexylamino-1-{3-[2-(4-fluoro-phenyl)-[1,3]dioxolan-2-yl]-propyl}-piperidine-4-carbonitrile 
• 169380-79-4 4-amino-1-{3-[2-(4-fluoro-phenyl)-[1,3]dioxolan-2-yl]-propyl}-piperidine-4-carbonitrile 

Relevant academic research and scientific papers

Spiperone: Influence of spiro ring substituents on 5-HT(2A) serotonin receptor binding

Spiperone (1) is a widely used pharmacological tool that acts as a potent dopamine D2, serotonin 5-HT(1A), and serotonin 5-HT(2A) antagonist. Although spiperone also binds at 5-HT(2C) receptors, it is one of the very few agents that display som

Synthesis of haloperidol ethanedithioketal HIV-1 protease inhibitors: Magnesium chloride facilitated addition of Grignard reagents

Haloperidol ketals and ethanedithioketals of interest as HIV-1 protease inhibitors were synthesized by addition of organolithium and organomagnesium reagents to ketone precursors already containing the ketal or thioketal functionality. Addition of Grignard reagents to the thioketal containing ketone was enhanced remarkably, and to the ketal containing ketone moderately, by the addition of magnesium chloride. The effect of magnesium chloride is attributed to its ability to competitively prevent chelation of the Grignard reagent and proton abstraction from the 4-oxopiperidine ring. The biological activities of the ketals and thioketals indicate that the thioketal function conveys greater ability to inhibit the HIV-1 protease than the ketal function.

Synthesis of [82Br]bromperidol and preliminary tissue distribution studies in the rat.

A procedure is described for the preparation of [82Br]bromperidol with specific activity 440 muCi/mg. The incorporation of bromine-82 into the molecule was accomplished through Brackman and Smit's modification of the Sandmeyer reaction, during the last step of the synthetic route. This involved the formation of a complex between Cu82Br2 and nitric oxide gas in acetonitrile, which was then allowed to react with 4-[4-(aminophenyl)-4-hydroxy-piperidinyl]-1-(4-fluorophenyl)-1-butanone (aminoperidol, 10) to give [82Br]bromperidol in about 1.5 h. Cupric 82Br]bromide was prepared in situ from K82Br and CuSO4.5H2O. The radiochemical and chemical yields for the preparation of [82Br]bromperidol from K82Br were 10.4 and 12%, respectively. Preliminary tissue distribution studies with the labeled bromperidol in the rat showed that the uptake of radioactivity by the liver, brain, kidneys, and the lungs was very fast and was in the declining phase in the latter organs 15 min after iv administration.

The synthesis of [14C]-labelled haloperidol and [d4]- and [d8] haloperidol

The synthesis of [14C] haloperidol for use in metabolism studies, and the synthesis of [d4]- and [d8] haloperidol for use in bioavailability studies, is described.