- Synthesis and biological activity of polyfluorinated p-aminosalicylic acids and their amides
-
Polyfluorinated analogues of salicylamide and p-aminosalicylic acid have been synthesized based on methyl polyfluorosalicylates. Polyfluorosalicylamides were obtained by the reaction with aqueous ammonia, while 4-aminopolyfluorosalicylic acids were prepar
- Burgart, Yanina V.,Saloutin, Victor I.,Shchegolkov, Evgeny V.,Shchur, Irina V.
-
p. 636 - 638
(2020/10/09)
-
- Preparation method of 3,4,5,6-tetrafluorosalicylic acid
-
The invention discloses a preparation method of 3,4,5,6-tetrafluorosalicylic acid. The preparation method comprises the following steps of adopting 2,3,4,5,6-pentafluorobenzoyl chloride as a raw material, obtaining intermediate products by condensation of the raw material with ethyl acetoacetate and complexation of the condensation products with cupric ions, and acidifying the intermediate products; obtaining 5,6,7,8-tetrafluoro-2-methyl-4-oxo-4H-benzopyran-3-carboxylic ethyl ester by cyclizaiton of the acidified products through heating, stirring the cyclization products in a sodium hydroxide solution, dropwise and slowly adding excessive amount of hydrogen peroxide solution, stirring and preserving the temperature of the mixture, and completing the reaction after the cyclization products are not detected by TLC; removing excessive amount of hydrogen peroxide by adding sodium thiosulfate, increasing the temperature for 1 hour, adjusting pH by adding hydrochloric acid after cooling the mixture to room temperature, and extracting target products with methyl tertiary butyl ether; drying the target products with anhydrous sodium sulfate, distilling the filter liquid, and obtaining 3,4,5,6-tetrafluorosalicylic acid by recrystallization of crude products by using dichloromethane. The preparation method has the advantages of low requirement for equipment, no pollution due to by-products of water, product recovery of 78-83% and crude product purity of 97%.
- -
-
Paragraph 0018; 0028; 0031
(2017/08/31)
-
- Polyfluorinated salicylic acid derivatives as analogs of known drugs: Synthesis, molecular docking and biological evaluation
-
We have developed the convenient methods for synthesis of polyfluorosalicylic acids and their derivatives. For the first time the biological properties of polyfluorosalicylates were investigated in vitro (permeability through the biological membranes, COX-1 inhibitory action) and in vivo (anti-inflammatory, analgesic activities, acute toxicity). Molecular docking of polyfluorinated salicylates confirmed in vitro and in vivo experiments.
- Shchegol'kov,Trefilova,Borisevich,Shchur,Ljushina,Khursan,Burgart, Ya.V.,Solodnikov, S.Yu.,Saloutin,Markova,Maslova,Krasnykh
-
-
- INHIBITORS OF STEAROYL-COA DESATURASE
-
Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity.
- -
-
-
- Selective ortho methoxylation of pentafluorobenzoic acid
-
Kinetics of reaction of pentafluorobenzoic acid with magnesium methoxide are studied. A new synthesis of tetrafluorosalicylic acid is developed. 3,4,5-Trifluoro-2,6-dimethoxybenzoic acid and 4,5,6-tri-ftororesorcinol and its dimethyl ether were first prepared.
- Bazyl',Kisil',Burgart,Kodess,Gein,Saloutin
-
p. 613 - 619
(2007/10/03)
-
- The selective ortho-methoxylation of pentafluorobenzoic acid - A new way to tetrafluorosalicylic acid and its derivatives
-
A simple and efficient preparation of tetrafluorosalicylic acid has been developed which involves a selective substitution of fluorine in pentafluorobenzoic acid with methoxyl group by magnesium methoxide. The synthesis of 2,6-dimethoxy-3,4,5-trifluorobenzoic acid, 4,5,6-trifluororesorcinol and its dimethoxy ether is described.
- Bazyl',Kisil',Burgart,Saloutin,Chupakhin
-
-
- Synthesis of long chain alkyl and chloroalkyl esters of perfluorosalicylic acid, new potential high temperature antifriction additives for advanced motor oils
-
Long chain alkyl and chloroalkyl esters of perfluorosalicyclic acid, which are potential antifriction additives for lubricating oil or fuel, are prepared by treating equimolar amounts of perfluorinated salicylic acid and a long chain alkyl alcohol in benzene in the presence of a strongly acidic ionic exchange resin.
- Sung, Kuangsen,Lagow, Richard J.
-
p. 917 - 918
(2007/10/03)
-
