- DEUTERIUM-ENRICHED SUBSTITUTED PHENOXYPHENYL ACETIC ACIDS AND ACYLSULFONAMIDES
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The present invention is concerned with deuterium-enriched substituted phenoxy-(3, 4-methylenedioxy)phenylacetic acid and acylsulfonamide derivatives of general structural formula I, their optically active or pure enantiomers and diastereomers, and pharmaceutical salts thereof, Formula (I) These compounds have selective antagonist activity for endothelin receptors or both endothelin and angiotensin II receptors, and are useful in the treatment of diseases mediated by endothelin and angiotensin-II and their receptors.
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Page/Page column 29; 31
(2021/06/22)
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- Synthesis method of (2,2-difluorobenzo[d][1,3]dioxy-5-yl)methanol
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The invention discloses a preparation method of (2,2-difluorobenzo[d][1,3]dioxo-5-yl)methanol as a fine chemical intermediate. The method is simple and feasible, lower in cost, and suitable for preparing (2,2-difluorobenzo[d][1,3]dioxo-5-yl)methanol through industrial production.
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- Synthesis of difluoroaryldioxoles using BrF3
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A novel synthesis of different aromatic and heteroaromatic difluorodioxole derivatives has been developed. The starting materials were catechols, which, after treatment with thiophosgene, formed at 0 °C the respective thiodioxoles. The latter were reacted for a short time with commercially available bromine trifluoride, producing potentially biologically important difluoroaryldioxoles in moderate to high yields.
- Hagooly, Youlia,Welch, Michael J.,Rozen, Shlomo
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p. 902 - 905
(2011/03/22)
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- Novel pharmaceutical compounds
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The present invention relates to derivatives of tadalafil, substituted with fluorine on the methylene carbon atom situated between the oxygens of the benzodioxol ring, and optionally further substituted with deuterium atoms in place of normally abundant hydrogen, and 13C in place of normally abundant 12C. These compounds are selective PDE5 inhibitors and possess advantageous biopharmaceutical and pharmacokinetic properties. The invention further provides compositions comprising these compounds and methods of treating diseases and conditions that are responsive to PDE5 inhibition, alone and in combination with additional agents.
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Page/Page column 20
(2010/11/25)
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- 2,2-difluorobenzo (1,3)-dioxole-carbaldehydes and new intermediate products
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According to the invention, a new process has been found for the preparation of 2,2-difluoro-benzo[1,3]-dioxole-carbaldehydes of the formula (I) STR1 in which benzo[1,3]dioxole-carbaldehydes are chlorinated, the 2,2-dichloro-dichloromethylbenzo[1,3]dioxoles formed, which are likewise new, are partly fluorinated to give the 2,2-difluoro-dichloromethyl-benzo[1,3]dioxoles, which are likewise new, and these are then reacted with urotropin to give the desired compounds.
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