期刊
APPLIED ORGANOMETALLIC CHEMISTRY
卷 34, 期 7, 页码 -出版社
WILEY
DOI: 10.1002/aoc.5650
关键词
acetylcholinesterase inhibitors; Arylsulfanyl-benzo-2; 1; 3-thiadiazole; cross-coupling; C-S bond
Functionalization of 2,1,3-benzothiadiazole (BTD) with thiols at C-5 position remains low explored. Moreover, the arylthiol-substitutions at this position are also unexplored and can not be found by a S(N)2 or S(N)1 reaction. In this sense, herein we present a new palladium-catalyzed methodology for a wide variety of unpublished 5-arylsulfanyl-benzo-2,1,3-thiadiazole derivatives synthesis with moderate to high yields using a low catalytic loading of Pd(L-Pro)(2) as low-coast, and efficient catalyst in low reaction time. Besides, we concluded that the pKa of thiol species has an important role in this catalysis, mainly in the CMD like catalytic cyclo process, which strongly interferes in the reaction yields. Furthermore, arylsulfanyl-benzo-2,1,3-thiadiazoles derivatives have been assessed (in vitro) as potential acetylcholinesterase inhibitors.
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