On December 2, 1999, Shirasawa, Eiichi; Konomi, Koji; Ichikawa, Masaki; Suhara, Hiroshi published a patent.Recommanded Product: 29704-38-9 The title of the patent was Preparation of novel 4-propenoylcinnamic acid or 1-propenoyl-4-(phosphonovinyl)benzene derivatives for treatment of glaucoma. And the patent contained the following:
Compounds represented by general formula (I) and salts thereof (wherein R1 is H, lower alkyl or Ph, the Ph being optionally substituted with lower alkyl, hydroxyl, lower alkoxy, halogeno, nitro or phenyl; R2 and R3 are each independently H, halogeno or lower alkyl; R4 and R5 are each independently H, lower alkyl or carboxyl, or a group derived therefrom through esterification; and R6 is carboxyl or phosphono, or a group derived from either through esterification), which decrease intraocular pressure based on the action similar to that of ethacrynic acid and are useful as glaucoma remedies, are prepared Thus, Et 4-carboxycinnamate was refluxed with SOCl2 in the presence of one drop of DMF in CHCl3 for 30 min and concentrated in vacuo to give the acid chloride. A 0.5 M solution of potassium bis(trimethylsilyl)amide in PhMe was added dropwise to a solution of tert-Bu 2,3,4,5,6-pentafluorophenylacetate in THF under dry ice-cooling and after 5 min, treated dropwise with a solution of the acid chloride in THF. In 20 min after completing the addition, the resulting mixture was stirred at room temperature for 20 min to give 4-[(2,3,4,5,6-pentafluorophenyl)acetyl]cinnamic acid which was heated with paraformaldehyde and dimethylamine hydrochloride in dioxane containing one drop of AcOH under stirring overnight to give the title compound (II) in 93% yield. When intracamerally injected in living monkeys, 4-(2-ethylacryloyl)cinnamic effected the greatest mean intraocular pressure reduction (7.0 mmHg) after 6 h vs. 2.0 mmHg for ethacrynic acid. The experimental process involved the reaction of tert-Butyl 2-(4-nitrophenyl)acetate(cas: 29704-38-9).Recommanded Product: 29704-38-9
The Article related to propenoylcinnamic acid preparation treatment glaucoma, propenoylphosphonovinylbenzene preparation treatment glaucoma, intraocular pressure reduction, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Carboxylic Acids and Peroxycarboxylic Acids and Their Sulfur-Containing Analogs and Salts and other aspects.Recommanded Product: 29704-38-9
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