The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: 1-(Bromomethyl)-4-iodobenzene(SMILESS: IC1=CC=C(CBr)C=C1,cas:16004-15-2) is researched.Product Details of 1265884-98-7. The article 《Synthesis and evaluation of new 1-oxa-8-azaspiro[4.5]decane derivatives as candidate radioligands for sigma-1 receptors》 in relation to this compound, is published in Bioorganic & Medicinal Chemistry. Let’s take a look at the latest research on this compound (cas:16004-15-2).
The design, synthesis, and evaluation of a series of 1-oxa-8-azaspiro[4.5]decane I (R = F, I, OCH2CH2F) and 1,5-dioxa-9-azaspiro[5.5]undecane derivatives II (R = F, I, OCH2CH2F, OMe) as selective σ1 receptor ligands has been reported. All seven ligands exhibited nanomolar affinity for σ1 receptors (Ki(σ1) = 0.47 – 12.1 nM) and moderate selectivity over σ2 receptors (Ki(σ2)/ Ki(σ1) = 2 – 44). Compound I (R = OCH2CH2F), with the best selectivity among these ligands, was selected for radiolabeling and further evaluation. Radioligand II (R = OCH2CH2F18) was prepared via nucleophilic 18F-substitution of the corresponding tosylate precursor, with an overall isolated radiochem. yield of 12-35%, a radiochem. purity of greater than 99%, and molar activity of 94 – 121 GBq/μmol. Biodistribution studies of II (R = OCH2CH2F18) in mice demonstrated high initial brain uptake at 2 min. Pretreatment with SA4503 resulted in significantly reduced brain-to-blood ratio (70% – 75% at 30 min). Ex vivo autoradiog. in ICR mice demonstrated high accumulation of the radiotracer in σ1 receptor-rich brain areas. These findings suggest that II (R = OCH2CH2F18) could be a lead compound for further structural modifications to develop potential brain imaging agents for σ1 receptors.
As far as I know, this compound(16004-15-2)Category: piperazines can be applied in many ways, which is helpful for the development of experiments. Therefore many people are doing relevant researches.
Reference:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics