Synthesis of a selective sigma receptor radioligand for SPECT: [123I]-1-(2-hydroxyethyl)-4-(4-iodophenoxymethyl)piperidine
摘要:
[I-123]-1-(2-Hydroxyethyl)-4-(4-iodophenoxymethyl) has been prepared as a novel sigma receptor radioligand for tumour imaging by SPECT. This ligand was found to be selective in vitro for the sigma-1 receptor (Ki = 2.3 nM) when tested in a variety of neuroreceptor binding assays. The lipophilicity of this ligand is appropriate for crossing the blood/brain barrier (log P-7.5 = 4.0) Radioiodination was accomplished by no-carrier-added iododestannylation using chloramine-T in acetic acid. The specific activity of the radiotracer >10,000 mCi/mu mole. The radiochemical yield was 63-77% EOS and the radiochemical purity was >99%.
Tetraarylphosphonium Salts as Soluble Supports for Oxidative Catalysts and Reagents
作者:Marie-Noelle Roy、Jean-Christophe Poupon、André B. Charette
DOI:10.1021/jo901509z
日期:2009.11.20
Tetraarylphosphonium (TAP)-supported DMSO, TEMPO, and DIB reagents were synthesized and used for the oxidation of alcohols, including Swern oxidation and for the α-acetoxylation of ketones. By taking advantage of the predictable solubility properties of the TAP unit, simple precipitation and filtration of the phosphonium moiety permit complete separation of the desired oxidation products. This paper