1202252-00-3Relevant academic research and scientific papers
Method for synthesizing benzothiazole derivatives
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, (2017/03/14)
The invention discloses a method for synthesizing benzothiazole derivatives. Thiourea is used as a sulfur source, and the thiourea and o-fluoronitrobenzene derivatives are continuously converted into the benzothiazole derivatives by means of three-step conversion. The method includes enabling 2-benzylthio-benzamide derivatives to react to trifluoroacetic acid and the thiourea to obtain reaction products, extracting the reaction products by the aid of n-hexane, concentrating n-hexane layers to obtain the benzothiazole derivatives, and adding the o-fluoronitrobenzene derivatives and sodium hydroxide solution into lower-layer water phases to obtain 2-benzylthio-nitrobenzene derivatives; reducing tin dichloride to obtain 2-benzylthio-aminobenzene derivatives; ultimately acylating the 2-benzylthio-aminobenzene derivatives to obtain 2-benzylthio-substituted benzamide analogs. The method has the advantages of simplicity, environmental protection and low cost.
A metal-free and recyclable synthesis of benzothiazoles using thiourea as a sulfur surrogate
Yin, Yan,Zhou, Hong,Liu, Xichen,Chen, Haiying,Wu, Fanhong,Zhang, Heng,Tao, Ruiheng,Cheng, Fengkai,Feng, Yangbo
, p. 1709 - 1712 (2015/03/14)
Using odorless thiourea as the S source, benzothiazoles and asymmetric disulfides could be obtained from thioformanilides through the tandem cyclization/nucleophilic addition/hydrolysis/nucleophilic substitution reaction. Furthermore, the obtained asymmetric disulfides could readily transfer to benzothiazoles after nitro-reduction and amide formation reaction. This metal-free and recyclable synthetic methodology offered a time-efficient, less expensive, and environmentally friendly alternative to multifunctional benzothiazoles.
Benzothiazoles as Rho-associated kinase (ROCK-II) inhibitors
Yin, Yan,Lin, Li,Ruiz, Claudia,Cameron, Michael D.,Pocas, Jennifer,Grant, Wayne,Schroeter, Thomas,Chen, Weimin,Duckett, Derek,Schuerer, Stephan,LoGrasso, Philip,Feng, Yangbo
scheme or table, p. 6686 - 6690 (2010/06/14)
A series of benzothiazole derivatives as ROCK inhibitors have been discovered. Compounds with good biochemical and cellular potency, and sufficient kinase selectivity have been identified.
