Discovery and optimization of a novel CNS penetrant series of mGlu4 PAMs based on a 1,4-thiazepane core with in vivo efficacy in a preclinical Parkinsonian model was written by Kent, Caitlin N.;Fulton, Mark G.;Stillwell, Kaylee J.;Dickerson, Jonathan W.;Loch, Matthew T.;Rodriguez, Alice L.;Blobaum, Anna L.;Boutaud, Olivier;Rook, Jerri L.;Niswender, Colleen M.;Conn, P. Jeffrey;Lindsley, Craig W.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2021.Application In Synthesis of 3-Fluoro-5-iodoaniline This article mentions the following:
A high throughput screen (HTS) identified a novel, but weak (EC50 = 6.2μM, 97% Glu Max) mGlu4 PAM chemotype based on a 1,4-thiazepane core, VU0544412. Reaction development and chem. optimization delivered a potent mGlu4 PAM VU6022296 (EC50 = 32.8 nM, 108% Glu Max) with good CNS penetration (Kp = 0.45, Kp,uu = 0.70) and enantiopreference. Finally, VU6022296 displayed robust, dose-dependent efficacy in reversing Haloperidol-Induced Catalepsy (HIC), a rodent preclin. Parkinson’s disease model. In the experiment, the researchers used many compounds, for example, 3-Fluoro-5-iodoaniline (cas: 660-49-1Application In Synthesis of 3-Fluoro-5-iodoaniline).
3-Fluoro-5-iodoaniline (cas: 660-49-1) belongs to iodide derivatives. Organic iodides can be alkyl, alkenyl, or alkynyl, and all of them are very reactive toward with many kinds of nucleophiles. A typical method for synthesis of aromatic iodides is diazotization of primary aromatic amines followed by treatment of potassium iodide. Aliphatic alcohols are converted to alkyl iodides by treating with hydrogen iodide.Application In Synthesis of 3-Fluoro-5-iodoaniline
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com