- IMPROVED PROCESS FOR THE PREPARATION OF CHLORTHALIDONE
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The present invention relates to methods for preparing chlorthalidone. In particular, the disclosed processes are feasible on an industrial scale and provide substantially pure chlorthalidone.
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Page/Page column 7
(2018/09/20)
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- Exploiting the Bis-Nucleophilicity of α-Aminoboronates: Copper-Catalyzed, Intramolecular Aminoalkylations of Bromobenzoyl Chlorides
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α-Aminoboronate salts are interesting examples of heteroatomic species containing adjacent nucleophilic centers. We have developed an acylation/arylation reaction using 2-bromobenzoyl chlorides as bis-electrophiles that harnesses the nucleophilicity of both positions, leading to isoindolinones. The reactions proceed under mild conditions via an intramolecular, Cu-catalyzed sp3-sp2 coupling, giving products in up to 95% yield. These conditions enable arylation of α,α-disubstituted aminoboronates, which are difficult to accomplish using methods based on less abundant and more expensive transition metals.
- Dumas, Aaron M.,Sieradzki, Adrian J.,Donnelly, Liam J.
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p. 1848 - 1851
(2016/05/19)
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- Study of the photochemical and in vitro phototoxicity of chlortalidone [2-chloro-5-(1-hydroxy-3-oxo-1-isoindolinyl)benzene sulfonamide]
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The photodegradation process of the phototoxic diuretic drag chlorthalidone was studied. The products of its photolysis under UV-B were isolated and identified. Chlorthalidone was found to be active when examined by photohemolysis on human erythrocytes, but not in the presence of the isolated photoproducts. Inhibition of the photohemolysis process induced by chlorthalidone on addition of reduced glutathione (GSH) or ascorbic acid suggests the involvement of radicals species. The inhibition with 1,4- diazabycyclo [2.2.2] octane (DABCO), sodium azide (NAN3) sowie 2,5- dimethylfuran proof the participation of singlet oxygen (1O2) in this process.
- Vargas, Franklin,Mendez
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p. 920 - 922
(2007/10/03)
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- Untersuchungen zur Chemie von Isoindolen und Isoindoleninen, XXXVIII. 3-Alkoxy-1H-isoindole mit Substituenten am 5-Ring - Heterocycliche Imidsaeureester mit fixierter benzoider Struktur.
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3-Alkoxy-1H-isoindoles bearing substituents at the five-membered ring have been synthesized starting with substituted isoindoline-1-ones via regiospecific O-alkylation with trialkyl oxonium tetrafluoroborates or alkyl trifluoromethanesulfonates and subsequent NH-deprotonation.The dependence of spectroscopic properties on the substituents has been investigated.The heterocyclic imidates exist exclusively in the benzenoid 1H-structure; the tautomeric o-quinonoid 2H-form cannot be detected by spectroscopic means.
- Kreher, Richard P.,Hennige, Hans,Konrad, Michael,Uhrig, Juergen,Clemens, Andrea
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p. 809 - 828
(2007/10/02)
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