Fluoroethoxy-1,4-diphenethylpiperidine and piperazine derivatives: Potent and selective inhibitors of [3H]dopamine uptake at the vesicular monoamine transporter-2 was written by Hankosky, Emily R.;Joolakanti, Shyam R.;Nickell, Justin R.;Janganati, Venumadhav;Dwoskin, Linda P.;Crooks, Peter A.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2017.Synthetic Route of C9H11BrO This article mentions the following:
A small library of fluoroethoxy-1,4-diphenethyl piperidine and fluoroethoxy-1,4-diphenethyl piperazine derivatives were designed, synthesized and evaluated for their ability to inhibit [3H]dopamine (DA) uptake at the vesicular monoamine transporter-2 (VMAT2) and dopamine transporter (DAT), [3H]serotonin (5-HT) uptake at the serotonin transporter (SERT), and [3H]dofetilide binding at the human-ether-a-go-go-related gene (hERG) channel. The majority of the compounds exhibited potent inhibition of [3H]DA uptake at VMAT2, Ki changes in the nanomolar range (Ki = 0.014-0.073 μM). Compound 1-(3-(2-Fluoroethoxy)phenethyl)-4-phenethylpiperazine exhibited the highest affinity (Ki = 0.014 μM) at VMAT2, and had 160-, 5-, and 60-fold greater selectivity for VMAT2 vs. DAT, SERT and hERG, resp. Compound 1-(3-(2-Fluoroethoxy)phenethyl)-4-phenethylpiperazine exhibited the greatest selectivity (>60-fold) for VMAT2 relative to all the other targets evaluated, and 1-(3-(2-Fluoroethoxy)phenethyl)-4-phenethylpiperazine had high affinity for VMAT2 (Ki = 0.073 μM). Compound 1-(3-(2-Fluoroethoxy)phenethyl)-4-phenethylpiperazine was considered the lead compound from this analog series due to its high affinity and selectivity for VMAT2. In the experiment, the researchers used many compounds, for example, 1-(2-Bromoethyl)-4-methoxybenzene (cas: 14425-64-0Synthetic Route of C9H11BrO).
1-(2-Bromoethyl)-4-methoxybenzene (cas: 14425-64-0) belongs to organobromine compounds. Bromo compounds are employed in a variety of metal-catalyzed coupling reactions. They are also ideal candidates for the synthesis of Grignard reagents that have wide-applicability in organic synthesis. alpha-Bromoesters are employed in the Reformatsky reaction for the synthesis of beta-hydroxyesters. In the pharmaceutical industry organo bromine derivatives are used as sedatives, vasodilators, antiseptic agents, and anticancer agents.Synthetic Route of C9H11BrO
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary