𝔖 Bobbio Scriptorium
✦   LIBER   ✦

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

✍ Scribed by Xiao-Shu He; Kan Sam Lee; Daniel Weinberger; Brian R. de Costa

Publisher
John Wiley and Sons
Year
1993
Tongue
French
Weight
408 KB
Volume
33
Category
Article
ISSN
0022-2135

No coin nor oath required. For personal study only.

✦ Synopsis

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 selective AIH~3~‐mediated reduction of 1[2‐(diphenylmethoxy)ethyl‐4‐(m‐bromocinnamoyl] piperazine (4) to 1‐[2‐(diphenylmethoxy)ethyl‐4‐(3‐(m‐bromophenyl)‐2‐propenyl]piperazine(5). The ^123^I label of [^123^I]2 was introduced in the final step in up to 90% radiochemical yield by treatment of the organotin precursor 1‐(2‐(diphenylmethoxy)ethyl‐4‐[3‐[(m‐(tributyl stannyl)phenyl]‐2‐propenyl]piperazine (6) with Na^123^I in aqueous CH~3~CO~3~H.

📜 SIMILAR VOLUMES

Synthesis of L-6-[123I]iodo-m-tyrosine a
Synthesis of L-6-[123I]iodo-m-tyrosine a potential spect brain imaging agent
✍ Michael J. Adam; Yolanda Zea Ponce; Joffre M. Berry 📂 Article 📅 1990 🏛 John Wiley and Sons 🌐 French ⚖ 295 KB 👁 1 views

## Abstract L‐6‐[^123^I]Iodo‐__m__‐tyrosine was synthesized by the direct iodination of L‐__m__‐tyrosine with [^123^I]‐NaI and Chloramine‐T. The product was purified by reverse phase HPLC to give the final product in 57% radiochemical yield with a radiochemical purity of greater than 97%.

Synthesis and preliminary evaluation of
Synthesis and preliminary evaluation of L-6-[123I]Iododopa as a potential spect brain imaging agent
✍ Michael J. Adam; Yolanda Zea Ponce; Joffre M. Berry; Kevin Hoy 📂 Article 📅 1990 🏛 John Wiley and Sons 🌐 French ⚖ 483 KB 👁 1 views

A bst rnct in buffer(pH 4) for 35 minutes at 97°C. The synthesis was complete in approximately 1 hour with a radiochemical yield of 50% , a specific activity of 65 Ci/mmol and a radiochemical purity of >95%. A non radioactive standard of L-6-iododopa was synthesized by the iododemercuration of a mer

4-123I - spiperone of high purity and hi
4-123I - spiperone of high purity and high specific activity. A suitable tracer for imaging dopamine receptor sites in baboon brains with spect
✍ J. Mertens; D. Terriere; A. Bossuyt; C. Bossuyt-Piron 📂 Article 📅 1989 🏛 John Wiley and Sons 🌐 French ⚖ 104 KB

Recently there has been an increased urge towards y-labelled tracers for in vivo dopamine receptors studies in human brain with SPECT. As 99m Tc chelate compunds for that purpose remain wishfull thinking until now, only 123 I labelled molecules can actually fulfil the technical requirements of imagi

Synthesis and biological evaluation of i
Synthesis and biological evaluation of iodine-125 iodocaramiphen. A potential M1 muscarinic imaging agent for SPECT
✍ Daniel W. McPherson; F. F. (Russ) Knapp Jr.; Robert L. Hudkins 📂 Article 📅 1994 🏛 John Wiley and Sons 🌐 French ⚖ 376 KB 👁 1 views

## Abstract Iodocaramiphen (2) is a selective muscarinic antagonist which binds __in vitro__ with high affinity and selectivity to the M~1~ subtype of the muscarinic receptor. We report the synthesis of iodine‐125 labeled iodocaramiphen ([^125^I]‐2) via a tributylstannyl intermediate (3) in 50% rad