64820-41-3Relevant academic research and scientific papers
Design, synthesis, and antiviral activities of 1,5-benzothiazepine derivatives containing pyridine moiety
Li, Tianxian,Zhang, Jian,Pan, Jianke,Wu, Zengxue,Hu, Deyu,Song, Baoan
supporting information, p. 657 - 662 (2016/10/14)
In our previous work, a series of novel benzothiazepine derivatives containing pyridine moiety were successfully synthesized through chalcone 1,3-dipolar cycloaddition and determined their antiviral activity against tobacco mosaic virus (TMV). Bioassay results indicated that most of these target compounds exhibited improved curative, protection, and inactivation activity in?vivo than the commercial agent ningnanmycin. Particularly, compound 3m exhibited marked curative activity against TMV, with an EC50value of 352.2?μM, which was even better than that of ningnanmycin. The compound was identified as the most promising candidate for inhibiting plant virus and an excellent compound with antiviral activities against TMV. Structure–activity relationship experiment indicated that the 1,5-benzothiazepine moiety is crucial for potent anti-TMV activity.
Pyridine-containing benzothiazepine derivatives, and preparation method and application thereof
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, (2016/10/10)
The invention discloses pyridine-containing benzothiazepine derivatives, and a preparation method and application thereof. The general formula (I) of the derivatives is described in the specification. In the formula (I), R is selected from a group consisting of a phenyl group, a 4-methylphenyl group, a thien-2-yl gourp, a 4-methoxyphenyl group, a 4-nitrophenyl group, a 4-trifluoromethoxyphenyl group, a 4-bromophenyl group, a furan-2-yl group, a 4-fluorophenyl group, a 3,4-dimethyoxyphenyl group, a 2-chlorophenyl group, a 2-phenyl group, a 3-bromophenyl group, a 2-methyoxyphenyl group, a 2-fluorophenyl group, a 3-methyoxyphenyl group, a 4-trifluoromethylphenyl group, a 2-trifluoromethylphenyl group, a 4-chlorophenyl group, a 3-fluorophenyl group, a 2,4-dichlorophenyl group, a 3,4-dichlorophenyl group, a 2,6-dichlorophenyl group, a 2-chloro-6-fluorophenyl group, a 3-nitrophenyl group and a naphtha-1-yl group. According to the invention, synthesis route is simple; yield is high; and plant virus diseases can be efficiently and safely prevented and controlled.
Facile synthesis of 1,5-benzothiazepines in water using tetrabutylammonium tribromide
Yan, Yunhui,Yang, Xiaojuan,Wu, Liqiang
experimental part, p. 573 - 579 (2012/06/01)
A simple, environmentally benign, and efficient method was developed for the preparation of 1,5-benzothiazepines via a one-pot condensation reaction of 2-aminothiophenol with 1,3-diaryl-2-propenones using tetrabutylammonium tribromide as an efficient and versatile catalyst in water.
An efficient synthesis of 1,5-benzothiazepines in the presence of sub-stoichiometric amount of cyanuric chloride
Sun, Pengli,Fang, Lizheng,Wu, Liqiang
experimental part, p. 257 - 261 (2012/01/03)
An efficient synthesis of 1,3-diaryl-2,3-dihydro-1,5-benzothiazepines has been developed by the reaction of various 1,3-diaryl-2-propenones with 2-aminothiophenol under thermal solvent-free conditions in the presence of a sub-stoichiometric amount of cyanuric chloride.
Synthesis of 1,5-benzothiazepines with microwave irradiation under solvent and catalyst-free conditions
Rahman,Roy,Majee,Hajra
experimental part, p. 178 - 179 (2010/02/28)
Microwave irradiation of a,β-unsaturated ketones (chalcones) and o-aminothiophenol in the absence of solvent and catalyst provides a highly efficient methodology for the synthesis of 1,5-benzothiazepines in moderate to good yields.
Ga(OTf)3-promoted condensation reactions for 1,5-benzodiazepines and 1,5-benzothiazepines
Pan, Xiang-Qiang,Zou, Jian-Ping,Huang, Zhi-Hao,Zhang, Wei
, p. 5302 - 5308 (2008/12/22)
Condensation reactions of o-phenylenediamine and two equivalents of acetophenone under gallium(III) triflate catalysis produce biaryl-substituted 1,5-benzodiazepines. Similar reactions of o-phenylenediamine or o-aminothiophenol and o-hydroxy chalcones lead to formation of functionalized 1,5-benzodiazepines and 1,5-benzothiazepines in good to excellent yields. The ortho-hydoxy group of chalcones is crucial for this unprecedented condensation process.
Magnesium perchlorate as a new and highly efficient catalyst for the synthesis of 2,3-dihydro-1,5-benzothiazepines
Khatik, Gopal L.,Kumar, Raj,Chakraborti, Asit K.
, p. 541 - 546 (2007/12/29)
Commercially available magnesium perchlorate has been found to be a highly efficient catalyst for the reaction of 1,3-diarylprop-2-enones with 2-aminothiophenol leading to the synthesis of 2,3-dihydro-1,5-benzothiazepines in high yields and in short times. Georg Thieme Verlag Stuttgart.
