Exploring the Neuroleptic Substituent in Octoclothepin: Potential Ligands for Positron Emission Tomography with Subnanomolar Affinity for α1-Adrenoceptors was written by Kristensen, Jesper L.;Puschl, Ask;Jensen, Martin;Risgaard, Rune;Christoffersen, Claus T.;Bang-Andersen, Benny;Balle, Thomas. And the article was included in Journal of Medicinal Chemistry in 2010.Safety of 5-Iodo-1-methyl-1H-pyrazole This article mentions the following:
A series of 1-(10,11-dihydrodibenzo[b,f]thiepin-10-yl)-4-methylpiperazines I (R = Cl, CN, Ph, 4-pyridyl, 1-methyltetrazol-5-yl, H2NCH2, MeCONHCH2, etc.) substituted in the 8-position of the 10,11-dihydrodibenzo[b,f]thiepine scaffold with aryl, heteroaryl, amine, and amide substituents is described. The compounds were designed using the previously reported Liljefors-Bogeso pharmacophore model for dopamine D2 and α1-adrenoceptor antagonists, with the aim of obtaining selective α1-adrenoceptor antagonists suitable for development as radioligands for imaging of central α1-adrenoceptors by positron emission tomog. Sixteen aryl and heteroaryl substituted octoclothepin analogs were prepared by a convergent synthesis via coupling of I (R = 4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl) with aryl and heteroaryl halides under palladium catalysis. The most selective compound obtained, (S)-I (R = i-PrCONHCH2), showed a similar subnanomolar affinity compared to α1a, α1b, and α1d-adrenoceptors and a selectivity ratio of 20, 440, and 20 with respect to D2, 5-HT2C, and H1 receptors, resp. In the experiment, the researchers used many compounds, for example, 5-Iodo-1-methyl-1H-pyrazole (cas: 34091-51-5Safety of 5-Iodo-1-methyl-1H-pyrazole).
5-Iodo-1-methyl-1H-pyrazole (cas: 34091-51-5) belongs to iodide derivatives. Organoiodine compounds occur widely in organic chemistry, but are relatively rare in nature. The C–I bond is the weakest of the carbon–halogen bonds. These bond strengths correlate with the electronegativity of the halogen, decreasing in the order F > Cl > Br > I. This periodic order also follows the atomic radius of halogens and the length of the carbon-halogen bond.Safety of 5-Iodo-1-methyl-1H-pyrazole
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com