ChemInform Abstract: Rapid Synthesis of Aliphatic Amides by Reaction of Carboxylic Acids, Grignard Reagent, and Amines: Application to the Preparation of [¹¹C]Amides.

Abstract

1998 amide formation, amide hydrolysis amide formation, amide hydrolysis O 0320 -058Rapid Synthesis of Aliphatic Amides by Reaction of Carboxylic Acids, Grignard Reagent, and Amines: Application to the Preparation of [ 11 C]Amides.-Grignard reagents promote the reaction of simple carboxylic acids with aliphatic amines. The amides (III) are obtained in moderate to good yields in a short time (5-60 min). The reaction conditions are successfully applied to the synthesis of 11 C-labeled amides. -(AUBERT, C.; HUARD-PERRIO, C.; LASNE, M.-C.; J.

Imaging Cholinergic Receptors in the Brain by Positron Emission Tomography

“…[ 11 C]BIBN99 (26) was obtained with a decay-corrected yield of 26% from [ 11 C]ethyl iodide, but to date, no studies have been conducted to investigate its potential use as a PET imaging agent. 99 Despite sharing similar chemical structures with several reported M1selective PET ligands, such as [ 11 C]xanomeline (18) and [ 11 C]butylthio-TZTP (19), [ 18 F]FP-TZTP (27) proved to exhibit higher binding affinity for M2 receptors (K i = 2.2 nM) in comparison to M1 receptors (K i = 7.4 nM). 100 The selectivity was confirmed through ex vivo ARG studies in knockout mice 101 as well as in vitro studies in muscarinic receptor-expressing cells and rat brain sections, which suggest that the slower dissociation kinetics of [ 18 F]FP-TZTP (27) from M2 receptors may be responsible for this selectivity.…”