40771-41-3Relevant articles and documents
Grignard-Reagent-Promoted Desulfonylation/Intramolecular Coupling for the Synthesis of 2-(1-Fluorovinyl)pyridines
Jiang, Gaoxi,Kang, Lei,Qian, Jinlong,Yang, Huameng,Zhang, Jinlong
supporting information, p. 9118 - 9122 (2020/12/02)
A novel process involving Grignard-reagent-promoted desulfonylation/intramolecular coupling of readily available α-fluoro-α,β-unsaturated-(2-pyridyl)sulfones was realized that provided a series of polysubstituted 2-(1-fluorovinyl)pyridines in good yields. The intrinsic coordination between pyridine and Mg(II) along with the "negative fluorine effect"of the substrates should play the key role for the smooth transformation in the absence of transition-metal catalysts.
IF5 affects the final stage of the Cl-F exchange fluorination in the synthesis of pentafluoro-λ6-sulfanyl-pyridines, pyrimidines and benzenes with electron-withdrawing substituents
Cui, Benqiang,Kosobokov, Mikhail,Matsuzaki, Kohei,Tokunaga, Etsuko,Shibata, Norio
supporting information, p. 5997 - 6000 (2017/07/10)
A difficult chlorine-fluorine (Cl-F) exchange fluorination reaction in the final stage of the preparation of pentafluoro-λ6-sulfanyl-(hetero)arenes having electron-withdrawing substituents has now been elucidated through the use of iodine pentafluoride. A major side-reaction of C-S bond cleavage was sufficiently inhibited by the potential interaction between F and I with a halogen bonding.
Discovery of MK-3168: A PET tracer for imaging brain fatty acid amide hydrolase
Liu, Ping,Hamill, Terence G.,Chioda, Marc,Chobanian, Harry,Fung, Selena,Guo, Yan,Chang, Linda,Bakshi, Raman,Hong, Qingmei,Dellureficio, James,Lin, Linus S.,Abbadie, Catherine,Alexander, Jessica,Jin, Hong,Mandala, Suzanne,Shiao, Lin-Lin,Li, Wenping,Sanabria, Sandra,Williams, David,Zeng, Zhizhen,Hajdu, Richard,Jochnowitz, Nina,Rosenbach, Mark,Karanam, Bindhu,Madeira, Maria,Salituro, Gino,Powell, Joyce,Xu, Ling,Terebetski, Jenna L.,Leone, Joseph F.,Miller, Patricia,Cook, Jacquelynn,Holahan, Marie,Joshi, Aniket,O'Malley, Stacey,Purcell, Mona,Posavecz, Diane,Chen, Tsing-Bau,Riffel, Kerry,Williams, Mangay,Hargreaves, Richard,Sullivan, Kathleen A.,Nargund, Ravi P.,DeVita, Robert J.
supporting information, p. 509 - 513 (2013/07/26)
We report herein the discovery of a fatty acid amide hydrolase (FAAH) positron emission tomography (PET) tracer. Starting from a pyrazole lead, medicinal chemistry efforts directed toward reducing lipophilicity led to the synthesis of a series of imidazole analogues. Compound 6 was chosen for further profiling due to its appropriate physical chemical properties and excellent FAAH inhibition potency across species. [11C]-6 (MK-3168) exhibited good brain uptake and FAAH-specific signal in rhesus monkeys and is a suitable PET tracer for imaging FAAH in the brain.