1383232-41-4Relevant academic research and scientific papers
A General Strategy for Site-Selective Incorporation of Deuterium and Tritium into Pyridines, Diazines, and Pharmaceuticals
Koniarczyk, J. Luke,Hesk, David,Overgard, Alix,Davies, Ian W.,McNally, Andrew
, p. 1990 - 1993 (2018)
Methods to incorporate deuterium and tritium atoms into organic molecules are valuable for medicinal chemistry. The prevalence of pyridines and diazines in pharmaceuticals means that new ways to label these heterocycles will present opportunities in drug design and facilitate absorption, distribution, metabolism, and excretion (ADME) studies. A broadly applicable protocol is presented wherein pyridines, diazines, and pharmaceuticals are converted into heterocyclic phosphonium salts and then isotopically labeled. The isotopes are incorporated in high yields and, in general, with exclusive regioselectivity.
Metal-free directed C?H borylation of 2-(N-methylanilino)-5-fluoropyridines and 2-benzyl-5-fluoropyridines
Chen, Lu,Ji, Yafei,Ma, Tao,Pang, Binghan,Wang, Shuai,Wu, Gaorong,Xu, Xiaobo
supporting information, (2021/11/04)
A novel method for metal-free C?H borylation of 2-(N-methylanilino)-5-fluoropyridines and 2-benzyl-5-fluoropyridines has been reported. The 5-fluoropyridine directed borylation reaction exhibited high efficiency and site exclusivity. The useful protocol could be executed on a gram-scale easily and the borylated products showed good derivatization applications. Moreover, the practicality of the strategy was expanded by the fact that the directing group could be removed in an acceptable yield.
Palladium-catalyzed oxidative alkynylation of arene C-H bond using the chelation-assisted strategy
Kim, Seok Hwan,Park, Sae Hume,Chang, Sukbok
supporting information; experimental part, p. 5162 - 5166 (2012/07/31)
Palladium-catalyzed alkynylation of arene C-H bonds with (triisopropylsilyl)acetylene was developed for the first time under oxidative conditions in the present study. Among various type of directing groups examined, the N-phenyl-2-aminopyridine skeleton was shown to be most effective and selective for the Pd-catalyzed direct alkynylation reaction, and the desired alkynylated products were obtained in moderate to good yields.
