当前位置: X-MOL 学术Beilstein. J. Org. Chem. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Synthesis of 1,4-benzothiazinones from acylpyruvic acids or furan-2,3-diones and o-aminothiophenol
Beilstein Journal of Organic Chemistry ( IF 2.2 ) Pub Date : 2020-09-21 , DOI: 10.3762/bjoc.16.193
Ekaterina E Stepanova , Maksim V Dmitriev , Andrey N Maslivets

Two synthetic approaches to enaminones fused to 1,4-benzothiazin-2-one moiety, which can be interesting in studies on biological activity, chemosensors, and fluorescence, were developed via the reaction of furan-2,3-diones or acylpyruvic acids in the presence of carbodiimides with o-aminothiophenols. The target enaminones were formed together with pharmaceutically interesting 2-hydroxy-2H-1,4-benzothiazin-3(4H)-ones. A selective synthetic approach to 2-hydroxy-2H-1,4-benzothiazin-3(4H)-ones was developed via the solvent-switchable reaction of furan-2,3-diones with o-aminothiophenol. Preliminary biological assays (antimicrobial, acute toxicity) of the new compounds were carried out.

中文翻译:

由酰基丙酮酸或呋喃-2,3-二酮和邻氨基苯硫酚合成1,4-苯并噻嗪酮

通过呋喃-2,3-二酮或酰基丙酮酸的反应,开发了两种与1,4-苯并噻嗪-2-酮部分融合的烯胺酮的合成方法,这在生物学活性,化学传感器和荧光研究中可能是有趣的。碳二亚胺与氨基苯硫酚的存在。目标烯胺酮与可药用的2-羟基-2 H -1,4-苯并噻嗪-3(4 H)-one一起形成。通过呋喃-2,3-二酮与氨基硫酚的溶剂转换反应,开发了选择性合成2-羟基-2 H -1,4-苯并噻嗪-3(4 H)-的方法。进行了新化合物的初步生物学测定(抗菌,急性毒性)。
更新日期:2020-09-21
down
wechat
bug