33429-11-7Relevant academic research and scientific papers
Photoinduced remote heteroaryl migration accompanied by cyanoalkylacylation in continuous flow
Duan, Xiu,Guo, Kai,Liu, Jie,Ma, Can-Liang,Qin, Long-Zhou,Qiu, Jiang-Kai,Sun, Qi,Wu, Meng-Yu,Yuan, Xin,Zhang, Xin-Peng,Zhu, Shan-Shan
supporting information, p. 8916 - 8921 (2021/11/27)
A photoinduced 1,4-heteroaryl migration from a carbon center to a nitrogen center accompanied by a cyanoalkylacylation of heterocyclic-substituted azidyl homoallylic alcohols and cycloketone oxime esters has been described. This simple and powerful protoc
C2 substituted 2H-benzothiazole aryl acylated derivative, and synthesis method and application thereof
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Paragraph 0029-0030, (2021/07/08)
The invention discloses a C2 substituted 2H-benzothiazole aryl acylated derivative, and a synthesis method and application thereof. The preparation method of the derivative comprises the following steps: mixing substituted 2H-benzothiazole and substituted methyl benzene, adding into a solvent, in the presence of an oxidizing agent Selectfluor and an additive trifluoroacetic acid, carrying out a heating and stirring reaction in the air atmosphere, performing TLC monitoring is conducted till the reaction is finished, and separating and purifying the obtained reaction liquid to obtain the target product C2 substituted 2H-benzothiazole aryl acylated derivative. The substituted methyl benzene used in the invention is low in price, easy to obtain and good in chemical stability, the method has the advantages of being high in atom economy, simple in catalytic system, free of transition metal catalysts, good in product yield, wide in substrate range and the like, and the prepared compound structure can be further optimized as an anti-tumor drug lead.
C2-arylacylation of 2H-benzothiazoles with methyl arenes via Selectfluor oxidation
Chen, Bo,Kong, Yao-Lei,Liu, Jin-Chuan,Lu, Qi,Sun, Xiao-Tong,Weng, Jian-Quan
supporting information, (2021/06/03)
An efficient Selectfluor-oxidative protocol was developed for the direct C2-arylacylation of 2H-benzothiazoles via the radical reaction of 2H-benzothiazoles with methyl arenes. Selectfluor can effectively promote the oxidative cross-coupling without an ex
Microwave-assisted controllable synthesis of 2-acylbenzothiazoles and bibenzo[b][1,4]thiazines from aryl methyl ketones and disulfanediyldianilines
Qi, Yuquan,Gu, Xiaoyu,Huang, Xianqiang,Shen, Guodong,Yang, Bingchuan,He, Qingpeng,Xue, Zechun,Du, Mengcheng,Shi, Lilong,Yu, Bing
supporting information, p. 3544 - 3547 (2021/07/02)
A condition-controlled strategy for selectively synthesis of 2-acylbenzothiazoles and bibenzo[b][1,4]thiazines from aryl methyl ketones and disulfanediyldianilines was realized using I2/DMSO or I2/MeCN systems, respectively. The desired products were synthesized in only 15 min with moderate to excellent yields (50%-90%) under microwave-assisted, metal-free conditions. The strategy provides a great advantage for selective synthetic applications in the efficient synthesis of benzothiazoles and bibenzothiazines heterocycle compounds.
Visible-light-promoted photocatalyst-free alkylation and acylation of benzothiazoles
Jiang, Pengxing,Liu, Li,Tan, Jiajing,Du, Hongguang
supporting information, p. 4487 - 4491 (2021/05/31)
Herein we report a protocol for the visible-light-mediated alkylation/acylation reaction of benzothiazoles. Alkyl/acyl substituted Hantzsch esters are easily prepared and rationally used as radical precursors. In the presence of BF3·Et2O and Na2S2O8, various benzothiazole derivatives were readily obtained in good yields. Our user-friendly protocol can proceed by simple irradiation with blue LEDs (λ = 465 nm) and without the assistance of external photocatalysts. The reaction is also characterized by mild conditions and scalability, thus offering an alternative and efficient tool for the synthesis of 2-functionalized benzothiazoles.
Preparation method of C2 substituted 2H-benzothiazole acylation derivative
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Paragraph 0020-0021, (2020/11/22)
The invention discloses a preparation method of a C2 substituted 2Hbenzothiazole acylation derivative. The preparation method comprises the following steps: mixing 2Hbenzothiazole with substituted methyl benzene, adding an oxidizing agent K2S2O8, reacting in an air atmosphere, carrying out TLC (Thin Layer Chromatography) monitoring until the reaction is finished, and separating and purifying the reaction solution to obtain the C2 substituted 2Hbenzothiazole acylation derivative. By the adoption of the technology, K2S2O8 serves as an oxidizing agent, the C2-substituted 2Hbenzothiazole acylationderivative is synthesized through a heating reaction in the air atmosphere, and the method is simple in catalytic system, good in product yield, wide in substrate range and suitable for application and popularization.
New synthesis of 2-aroylbenzothiazolesviametal-free domino transformations of anilines, acetophenones, and elemental sulfur
Doan, Khang V.,Doan, Son H.,Huynh, Tien V.,Luong, Ngoc T. K.,Nguyen, Duyen T. P.,Nguyen, Tung T.,Phan, Nam T. S.
, p. 18423 - 18433 (2020/06/08)
A new synthesis of 2-aroylbenzothiazolesviaiodine-promoted domino transformations of anilines, acetophenones, and elemental sulfur was demonstrated. The highlights of this tandem synthesis are (1) easily available anilines and acetophenones as feedstock;
Method for simply and conveniently synthesizing heterocyclic aryl ketone compound
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Paragraph 0046; 0047; 0048; 0049; 0050; 0053, (2019/01/23)
The invention discloses a method for simply and conveniently synthesizing a heterocyclic aryl ketone compound, and belongs to the technical field of the organic chemistry. The method comprises the following steps: using a benzyl heterocyclic compound as a reaction raw material, in a polar solvent, heating and reacting in an oxygen atmosphere, to obtain a multi-substituted ketone compound. The method is capable of using molecular oxygen as an oxidizing agent, green and environmental, and capable of preparing ketone by directly promoting selective oxidation and functionalization of a Csp3-H bond, and broadening a synthetic method for the ketone compound.
Elemental sulfur mediated 2-substituted benzothiazole formation from 2-aminobenzenethiols and arylacetylenes or styrenes under metal-free conditions
Li, Guozheng,Jiang, Jingjing,Zhang, Feng,Xiao, Fuhong,Deng, Guo-Jun
, p. 10024 - 10028 (2017/12/26)
An oxidative cyclization of 2-aminothiophenols and arylacetylenes or styrenes for the synthesis of 2-alkylbenzothiazoles and 2-acylbenzothiazoles has been developed. Elemental sulfur was used as the effective oxidant to give the corresponding product in g
Synthesizing method of medicine intermediate benzothiazole compound
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Paragraph 0048; 0049; 0050; 0051;, (2016/10/07)
The invention relates to a synthesizing method of a benzothiazole compound which is shown in the formula (III) (please see the formula in the specification) and can be used as medicine intermediate. The method includes the steps that a compound of the for
