292870-42-9Relevant academic research and scientific papers
Eine einfache Methode zur Herstellung von Benzoxazolen
Seha, Zdenek,Weis, Claus D
, p. 413 - 419 (1980)
The preparation of benzoxazoles by a facile one-pot reaction is reported.The reaction of carboxylic acids with 2-chloro-N-methyl-Δ1-pyrrolinium chloride in an excess of N-methyl-2-pyrrolidone afforded carboxylic acid chlorides which were converted subsequently to their 2-hydroxyanilides by addition of 2-aminophenols.Cyclization of the 2-hydroxy-anilides at elevated temperatures furnished the benzoxazoles in high yield and purity.
Synthesis and structure-activity relationships of small-molecular di-basic esters, amides and carbamates as flaviviral protease inhibitors
Sundermann, Tom R.,Benzin, Clarissa V.,Dra?i?, Tonko,Klein, Christian D.
supporting information, p. 187 - 194 (2019/05/21)
Inhibitors of the flaviviral serine proteases, which are crucial for the replication of dengue and West-Nile virus, have attracted much attention over the last years. A dibasic 4-guanidinobenzoate was previously reported as inhibitor of the dengue protease with potency in the low-micromolar range. In the present study, this lead structure was modified with the intent to explore structure-activity relationships and obtain compounds with increased drug-likeness. Substitutions of the guanidine moieties, the aromatic rings, and the ester with other functionalities were evaluated. All changes were accompanied by a loss of inhibition, indicating that the 4-guanidinobenzoate scaffold is an essential element of this compound class. Further experiments indicate that the target recognition of the compounds involves the reversible formation of a covalent adduct.
METHOD FOR MANUFACTURING BENZOXAZOLE COMPOUNDS
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Paragraph 0028-0030, (2017/04/28)
A method for manufacturing benzoxazole compounds is provided and has steps of: processing a reaction between o-aminophenol or a derivative thereof and an acyl chloride compound, so as to obtain a first product; and adding the first product into a solution of polyphosphoric acid to carry out a cyclization, so as to form a benzoxazole compound.
