Strategies for the Production of [¹¹C]LY2795050 for Clinical Use

Abstract

This report describes a comparison of four different routes for the clinical-scale radiosynthesis of the κ-opioid receptor antagonist [11C]LY2795050. Palladium-mediated radiocyanation and radiocarbonylation of an aryl iodide precursor, as well as copper-mediated radiocyanation of an aryl iodide and an aryl boronate ester, have been investigated. Full automation of all four methods is reported, each of which provides [11C]LY2795050 in sufficient radiochemical yield, molar activity, and radiochemical purity for clinical use. The advantages and disadvantages of each radiosynthesis method are compared and contrasted.

Automated production of 11C‐labeled carboxylic acids and esters via “in‐loop” 11C‐carbonylation using GE FX synthesis modules

“…For semi-preparative HPLC purification, initially, we used a two-loop system by adding a dedicated reaction loop to the module so as to keep the original module HPLC loop for purification. 30 This setup was complicated, and loss of activity because of the extra transfer was observed. Thus, we designed a simplified configuration using only one HPLC loop for both reaction and semi-preparative HPLC purification.…”

A Molecular Toolbox of Positron Emission Tomography Tracers for General Anesthesia Mechanism Research

“…The PET image with [ 11 C]­Ro15-4513 ([ 11 C] 34 ) has been duplicated from ref , with permission from Wolters Kluwer Health, Inc. The PET image with [ 11 C]­LY2795050 ([ 11 C] 35 ) has been duplicated from ref , with permission from American Chemical Society. The PET image with [ 11 C]­DPN ([ 11 C] 37 ) has been duplicated from ref , with permission from Wolters Kluwer Health, Inc.…”