118055-19-9Relevant academic research and scientific papers
Highly diastereoselective synthesis of 3-methylenetetrahydropyrans by palladium-catalyzed oxa-[4 + 2] cycloaddition of 2-alkenylbenzothiazoles
Ni, Qijian,Song, Xiaoxiao,Xu, Lei
supporting information, p. 6617 - 6621 (2020/09/21)
A highly diastereoselective synthesis of 3-methylenetetrahydropyrans via palladium-catalyzed oxa-[4 + 2] cycloaddition of 2-alkenylbenzothiazoles with allyl carbonates bearing a nucleophilic alcohol side chain is presented. This synthetic methodology tolerates a wide variety of 2-alkenylbenzothiazoles and afforded the desired 3-methylenetetrahydropyrans in good yields and excellent dr. In addition, further derivatizations resulted in new scaffolds, making them useful synthetic precursors.
Design, Synthesis, and Anticancer Activity of Novel Benzothiazole Analogues
Hassan, Aisha Y.,Sarg, Marwa T.,Hussein, Ebtehal M.
, p. 1437 - 1457 (2019/03/07)
On the pharmaceutical account of the reported anticancer activity of benzothiazole derivatives, differently substituted benzothiazole derivatives 2a–c to 34a,b, attached at 2-position to different heterocyclic moieties, were synthesized via different chemical reactions. Thirteen of the newly synthesized compounds were selected by the National Cancer Institute, Bethesda, Maryland, USA, and evaluated for their in vitro antitumor activity against 60 human tumor cell lines in a one-dose screening panel among which two compounds 4 and 17 showed high activity and were selected for further evaluation in the five-dose full panel assay, in which compound 4 exerted powerful growth inhibitory activity against all cell lines with GI50 ranging from 0.683 to 4.66?μM/L in addition to excellent lethal activity against most of the cell lines.
Enantioselective Reaction between 2-(Cyanomethyl)azaarenes and N-Boc-amino Sulfones
Wang, Kezhou,Chen, Chao,Liu, Xihong,Li, Dan,Peng, Tianyu,Liu, Xin,Yang, Dongxu,Wang, Linqing
supporting information, p. 5260 - 5263 (2018/09/13)
A series of 2-(cyanomethyl)azaarenes containing benzothiazole or benzoxazole were designed and synthesized for asymmetric α-functionalization with N-Boc-amino sulfones. The Mannich adducts were obtained in high yields with good diastereo- and enantioselectivities. Aryl-substituted amino sulfones were tolerated under the current conditions, and the reaction can be performed on gram scale in good results.
A splendid method for synthesis of 2-(benzothiazole)-3-phenyl acrylonitrile derivatives catalysed by piperdine
Maddila, Suresh,Jonnalagadda, Sreekanth B.
, p. 467 - 471 (2012/10/29)
A simple and efficient method is developed for the synthesis of 2-(benzothiazol-2-yl)-3- (substituted phenyl)acrylonitrile from 2-(benzothiazole-2-yl)-3-oxopentanedinitrile and aromatic aldehydes in the presence of a catalytic amount of piperdine into ethanol at reflux. Advantage of this procedure is relatively good yields (81-86%) with short reaction times (1.5-3 h), under moderate reaction conditions and simple workup procedure, plus easy preparation and handling of the catalyst.
