Giancola, JoLynn B.’s team published research in European Journal of Medicinal Chemistry in 2020-12-15 | CAS: 73874-95-0

European Journal of Medicinal Chemistry published new progress about Alkylation. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Synthetic Route of 73874-95-0.

Giancola, JoLynn B. published the artcileStructure-activity relationships for a series of (Bis(4-fluorophenyl)methyl)sulfinylethyl-aminopiperidines and -piperidine amines at the dopamine transporter: Bioisosteric replacement of the piperazine improves metabolic stability, Synthetic Route of 73874-95-0, the main research area is aminopiperidine piperidine amine preparation dopamine transporter SAR; Atypical dopamine uptake inhibitors; Cocaine; DAT; Modafinil; NET; Psychostimulant use disorders; SERT; Sigma receptors.

The bioisosteric substitutions of the piperazine ring were explored with a series of aminopiperidines and piperidine amines wherein compounds with either a terminal tertiary amine or amide were synthesized. Several lead compounds showed high to moderate DAT affinities and metabolic stability in rat liver microsomes. N-(2-((bis(4-fluorophenyl)methyl)sulfinyl)ethyl)-1-(4-fluorobenzyl)piperidin-4-amine (DAT Ki = 50.6 nM), I [R= F] (DAT Ki = 77.2 nM) and II [X1=X2= F] (DAT Ki = 30.0 nM) produced only minimal stimulation of ambulatory activity in mice, compared to cocaine, suggesting an atypical DAT inhibitor profile.

European Journal of Medicinal Chemistry published new progress about Alkylation. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Synthetic Route of 73874-95-0.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem