Positively charged water-soluble prodrug of diflunisal and related compound
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A compound and active ingredient technology, applied in the field of prodrugs of positively charged water-soluble diflunisal and related compounds
Active Publication Date: 2016-03-30
TECHFIELDS BIOCHEM CO LTD
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However, it is difficult to achieve therapeutically effective plasma concentrations of diflunisal by means of formulations
Method used
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[0067] 1. the synthetic method of diethylaminoethyl salicylate salicylate acetate
[0068] 31.8 g (0.1 mol) of acetylsalicyloyl salicylic acid chloride were dissolved in 100 ml of chloroform. The mixture was cooled to 0 °C. 15 ml of triethylamine and 8.9 g (0.1 mol) of dimethylaminoethanol were added to the reaction mixture. The mixture was stirred at room temperature for 3 hours. The reaction solvent was distilled off. The residue was dissolved in 300 ml of methanol, and 200 ml of 5% aqueous sodium bicarbonate was added to the reaction mixture. The mixture was stirred for 3 hours. The mixture was evaporated to dryness, and 300 ml of methanol were added to the residue with stirring. The solid was removed by filtration and washed with methanol. The solution was evaporated to dryness, and 200 ml of chloroform was added to the residue. 6 g of acetic acid was added to the reaction mixture with stirring. The solids were removed by filtration. An additional 6 g of acetic ac...
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Abstract
The present invention relates to design and synthesis of a novel prodrug of diflunisal, salsalate, and salicylic acid, wherein the prodrug is positively charged, and has a structural formula 1 as shown in the general formula (1), and a structural formula 2 as shown in the general formula (2). The compound with the structural formula 1 as shown in the general formula (1), and the structural formula 2 as shown in the general formula (2) can be prepared by a reaction of diflunisal, salsalate and salicylic acid with appropriate alcohol, mercaptan, or amine. The prodrugs can be used in medicine for the therapy of humans or animals in a state that can be treated with diflunisal, salsalate, or salicylic acid, and in the therapy process, the prodrugs can be orally used, and can be transdermally administrated, so that the most side effects of the diflunisal, salsalate, or salicylic acid are avoided. According to a controlled release transdermal administration system of the prodrug, the concentration of the diflunisal, salsalate, or salicylic acid in blood can be kept stable in the optimal therapy proficiency, so that the efficacy is improved, and the side effects of the diflunisal, salsalate, or salicylic acid are reduced.
Description
[0001] This application is a divisional application of the Chinese invention patent application No. 200680055458.0. The filing date of the original application was July 26, 2006, and the title of the invention was "Prodrugs of Positively Charged Water-Soluble Diflunisal and Related Compounds with Rapid Skin Penetration Speed". technical field [0002] The present invention relates to positively charged water-soluble prodrugs of 5-(2,4-difluorophenyl)salicylic acid (diflunisal), salicylsalicylic acid or other salicylic acid analogues and their use in the treatment of Any use of diflunisal, salicylsalicylic acid and salicylic acid in treating diseases in humans or animals. Specifically, the present invention aims to overcome the side effects caused by the use of diflunisal, salicyl salicylate or salicylic acid. These prodrugs can be administered orally or transdermally. technical background [0003] Diflunisal and salicyl salicylic acid are two of many salicylic acid NSAI...
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