3973-09-9Relevant articles and documents
Site-Selective and Stereoselective C(sp3)-H Borylation of Alkyl Side Chains of 1,3-Azoles with a Silica-Supported Monophosphine-Iridium Catalyst
Murakami, Ryo,Iwai, Tomohiro,Sawamura, Masaya
, p. 1187 - 1192 (2016)
Site-selective and stereoselective C(sp3)-H borylation of alkyl side chains of 1,3-azoles with bis(pinacolato)diboron was effectively catalyzed by a silica-supported monophosphine-iridium catalyst. The borylation occurred under relatively mild conditions (2 mol% Ir, 50-90 °C), affording the corresponding primary and secondary alkylboronates. This system was applicable to a variety of 1,3-(benzo)azoles such as thiazoles, oxazoles, and imidazoles.
HYDROXYL PURINE COMPOUNDS AND USE THEREOF
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, (2018/04/05)
Disclosed are a series of hydroxyl purine compounds and the use thereof as PDE2 or TNFα inhibitors, in particular, the compounds as shown in formula (I), or tautomers thereof or pharmaceutically acceptable salts thereof.
TEMPO-Catalyzed Electrochemical C-H Thiolation: Synthesis of Benzothiazoles and Thiazolopyridines from Thioamides
Qian, Xiang-Yang,Li, Shu-Qi,Song, Jinshuai,Xu, Hai-Chao
, p. 2730 - 2734 (2017/05/31)
Benzothiazoles and thiazolopyridines are widely prevalent in pharmaceuticals and organic materials. Herein, we report a metal- and reagent-free method for the uniform synthesis of benzothiazoles and thiazolopyridines through 2,2,6,6-tetramethylpiperidine-N-oxyl radical (TEMPO)-catalyzed electrolytic C-H thiolation. This dehydrogenative coupling process provides access to a host of benzothiazoles and thiazolopyridines from N-(hetero)arylthioamides. Mechanistic studies suggested that the thioamide substrate was oxidized with the electrochemically generated TEMPO+ through an inner-sphere electron transfer to afford a thioamidyl radical, which undergoes homolytic aromatic substitution to form the key C-S bond.