✦ LIBER ✦

Synthesis of [18F]GBR 12909, a dopamine reuptake inhibitor

✍ Scribed by Michael S. Haka; Michael R. Kilbourn

Publisher: John Wiley and Sons
Year: 1990
Tongue: French
Weight: 304 KB
Volume: 28
Category: Article
ISSN: 0022-2135
DOI: 10.1002/jlcr.2580280708

No coin nor oath required. For personal study only.

✦ Synopsis

Abstract

Preparation of no‐carrier‐added fluorine‐18 labeled GBR 12909 (1‐[2‐(bis(4‐fluorophenyl)methoxy)ethyl]‐4‐(3‐phenylpropyl)piperazine), a specific and high affinity inhibitor of dopamine reuptake, is described. 4‐Fluoro‐4′‐[^18^F]fluorobenzophenone was prepared by [^18^F]fluoride ion substitution of the corresponding trimethylammonium trifluoromethanesulfonate salt. The [^18^F]benzophenone was reduced to the benzhydrol, chlorinated, then used to alkylate 1‐(2‐hydroxyethyl)‐4‐(3‐phenyl‐propyl)piperazine to yield [^18^F]GBR 12909 in high specific activity (≥2000 Ci/mmol) and overall yields of 10–16% (corrected, 140 min synthesis).

📜 SIMILAR VOLUMES

ChemInform Abstract: Synthesis and Evalu

ChemInform Abstract: Synthesis and Evaluation of Novel N-[2-(bisarylmethoxy)ethyl]-N′-aralkyl-α,ω-alkanediamines as Potent and Selective Dopamine Reuptake Inhibitors: seco Analogues of GBR12935 and GBR12909.

✍ R. N. HANSON; S.-W. CHOI; D. R. ELMALEH; A. J. FISCHMAN 📂 Article 📅 2010 🏛 John Wiley and Sons ⚖ 37 KB

ChemInform Abstract: Development of Nove

ChemInform Abstract: Development of Novel, Potent, and Selective Dopamine Reuptake Inhibitors Through Alteration of the Piperazine Ring of 1-(2-( Diphenylmethoxy)ethyl)- and 1-(2-(Bis(4-fluorophenyl)methoxy)ethyl)-4-( 3-phenylpropyl)piperazines (GBR 12935 and GBR 12909).

✍ D. MATECKA; R. B. ROTHMAN; L. RADESCA; B. R. DE COSTA; C. M. DERSCH; J. S. PARTI 📂 Article 📅 2010 🏛 John Wiley and Sons ⚖ 39 KB 👁 1 views

Synthesis of a novel 123I-labelled deriv

Synthesis of a novel 123I-labelled derivative of GBR12783, a potential agent for SPECT imaging of dopamine-reuptake sites

✍ Xiao-Shu He; Kan Sam Lee; Daniel Weinberger; Brian R. de Costa 📂 Article 📅 1993 🏛 John Wiley and Sons 🌐 French ⚖ 408 KB

## Abstract [^123^I]1‐[2‐(Diphenylmethoxy)ethyl]‐4‐[3‐(__m__‐iodophenyl)‐2‐propenyl]piperazine ([^123^I]2), a potential SPECT imaging agent for dopamine reuptake sites was efficiently synthesized in 4 steps from 1‐[2‐(diphenylmethoxy)ethyl]piperazine (3). A key step in the synthesis was the selecti

ChemInform Abstract: Synthesis of a Pote

ChemInform Abstract: Synthesis of a Potent Wide-Spectrum Serotonin-, Norepinephrine-, Dopamine-Reuptake Inhibitor (SNDRI) and a Species-Selective Dopamine-Reuptake Inhibitor Based on the Gamma-Amino Alcohol Functional Group.

✍ P. R. CARLIER; M. M.-C. LO; P. C.-K. LO; E. RICHELSON; M. TATSUMI; I. J. REYNOLD 📂 Article 📅 2010 🏛 John Wiley and Sons ⚖ 31 KB 👁 2 views

Aryltrimethylammonium trifluoromethanesu

Aryltrimethylammonium trifluoromethanesulfonates as precursors to aryl [18F]fluorides: Improved synthesis of [18F]GBR-13119

✍ Michael S. Haka; Michael R. Kilbourn; G. Leonard Watkins; Steven A. Toorongian 📂 Article 📅 1989 🏛 John Wiley and Sons 🌐 French ⚖ 444 KB

Aromatic nucleophilic substitution of various trimethylammonium trifluoromethanesulfonates with [18F]fluoride has been evaluated. Fluorinations were studied over a temperature range of 45-165"C, with decay corrected yields ranging from 20-80%. [ I 8F]GBR 131 19, 1-[2-[(4-[~~F]fluorophenyl)(phenyl)me

Novel Feature Extraction Technique for F

Novel Feature Extraction Technique for Fuzzy Relational Clustering of a Flexible Dopamine Reuptake Inhibitor.

✍ Milind Misra; Amit Banerjee; Rajesh N. Dave; Carol A. Venanzi 📂 Article 📅 2005 🏛 John Wiley and Sons ⚖ 8 KB