In 2011,Liu, Jingying; Zhu, Lin; Ploessl, Karl; Lieberman, Brian P.; Kung, Hank F. published 《Synthesis and evaluation of novel N-fluoropyridyl derivatives of tropane as potential PET imaging agents for the dopamine transporter》.Bioorganic & Medicinal Chemistry Letters published the findings.Product Details of 13534-97-9 The information in the text is summarized as follows:
A series of novel N-fluoropyridyl-containing tropane derivatives, e.g., I, were synthesized and their binding affinities for the dopamine transporter (DAT), serotonin transporter (SERT) and norepinephrine (NET) were determined via competitive radioligand binding assays. Among these derivatives, compound I showed the highest binding affinity to DAT (Ki = 4.1 nM), and selectivity for DAT over SERT (5-fold) and NET (16-fold). Compound I was radiolabeled with Fluorine-18 in two steps. Regional brain distribution and ex vivo autoradiog. studies of [18F]I demonstrated that the ligand was selectively localized in the striatum region, where DAT binding sites are highly expressed. [18F]I may be useful as a potential radioligand for imaging DATs with PET. The experimental part of the paper was very detailed, including the reaction process of 6-Bromopyridin-3-amine(cas: 13534-97-9Product Details of 13534-97-9)
6-Bromopyridin-3-amine(cas: 13534-97-9) belongs to anime. Hydrogen peroxide (H2O2) and peroxy acids generally add an oxygen atom to the nitrogen of amines. With primary amines, this step is normally followed by further oxidation, leading to nitroso compounds, RNO, or nitro compounds, RNO2. Secondary amines are converted to hydroxylamines, R2NOH, and tertiary amines to amine oxides, R3NO.Product Details of 13534-97-9