73344-39-5Relevant academic research and scientific papers
A kind of benzo [d] different wicked zuozuo apperception compound and use thereof
-
, (2018/06/14)
The invention relates to the technical field of chemical medicine, and particularly discloses a benzo[d]isoxazole compound shown as a general formula (A) and application thereof. The compound can effectively inhibit bromodomain of BET family proteins so as to block interaction between the BET family proteins and chromatin histone to adjust genetic transcription, cause changing of a downstream signal path and exert important influence on various diseases, so that the compound and a combination thereof can be used for preparing medicine for treating or preventing diseases like tumorigenesis, inflammation, viral infection, cell proliferation disorder, autoimmune diseases and septicemia.
Method for preparing benzisoxazole in one pot based on 2-hydroxyacetophenone oxime and derivatives thereof
-
Paragraph 0018; 0019; 0020; 0036; 0037; 0038, (2017/08/24)
The invention relates to the technical field of medicinal chemistry and in particular discloses a method for preparing benzisoxazole in one pot based on 2-hydroxyacetophenone oxime and derivatives thereof. The preparation method is as follows: under microwave or oil bath heating conditions, in an organic solvent, one-pot inversion is carried out on 2-hydroxyacetophenone oxime and derivatives thereof to form benzisoxazole compounds by utilizing a fluorine-containing accelerator and alkali. The method for synthesizing benzisoxazole has the advantages that raw materials are rich in source and easy to get, synthetic steps are short, the operation is simple and convenient, the product yield is high, and the highest yield is 93%. A benzisoxazole structure exists in multiple drug molecules, so that the novel one-pot synthesis method disclosed by the invention has potential practical values.
A divergent and selective synthesis of isomeric benzoxazoles from a single N-Cl imine
Chen, Cheng-Yi,Andreani, Teresa,Li, Hongmei
, p. 6300 - 6303 (2012/01/05)
A divergent and regioselective synthesis of either 3-substituted benzisoxazoles or 2-substituted benzoxazoles from readily accessible ortho-hydroxyaryl N-H ketimines is described. The reaction proceeds in two distinct pathways through a common N-Cl imine intermediate: (a) N-O bond formation to form benzisoxazole under anhydrous conditions and (b) NaOCl mediated Beckmann-type rearrangement to form benzoxazole, respectively. The reaction path also depends on the electronic nature of the aromatic ring, with the electron-rich aromatic rings favoring the rearrangement and the electron-deficient rings favoring the N-O bond formation. A Beckmann-type rearrangement mechanism via net [1,2]-aryl migration for the formation of 2-substituted benzoxazole is proposed.
Antitubercular Agents: Part VI- Alkoxy Derivatives of 6-Hydroxy-3-methyl-1,2-benzisoxazole
Sahasrabudhe, A. B.,Kamath, S. V.,Bapat, B. V.,Bhawal, B. M.,Kulkarni, Sheshagiri N.
, p. 1266 - 1267 (2007/10/02)
Several alkoxy derivatives of 6-hydroxy-3-methyl-1,2-benzisoxazoles have been synthesised and screened for their antitubercular activity for QSAR studies.
