Endothelin receptor antagonists: synthesis and structure–activity relationships of substituted benzothiazine-1,1-dioxides

Polythienobenzothiophenes, a new family of electroactive polymers: electrosynthesis, spectral characterization and modelling

“…Based on the method of Ricci et al, 18 a new and efficient preparative synthesis of 1 and its 6-methoxy derivative 2 (MeOTBT) was elaborated. The starting thiosalicylic acid and 4-methoxythiosalicylic acid, 22 respectively, were alkylated with chloroacetic acid to afford diacids 3 and 4 (Scheme 2). Cyclization 23 of these diacids by means of N,N-dimethylformamide and phosphorus oxide chloride was followed by a subsequent formylation and chlorination leading to chloro aldehydes 5 and 6 in high yield.…”

Advances in the Chemistry of Saccharins: From Synthetic Novelties Towards Biologically Active Compounds

“…A different entry to the saccharin nucleus 34 was achieved by intramolecular sulfonylation/acylation of the corresponding derivatives 32 and 33 (Scheme 10) [23,24].…”

3-(3-Chlorobenzoyl)-4-hydroxy-2H-1,2-benzothiazine 1,1-dioxide

“…For the biological activity of 1,2-benzothiazine derivatives, see: Ahmad et al (2010); Lombardino & Wiseman, (1972); Gupta et al (1993Gupta et al ( , 2002; Zia-ur-Rehman et al (2006); Berryman et al (1998). For comparative bond distances, see: Allen et al (1987).…”

“…HLS is grateful to the Institute of Chemistry, University of the Punjab, for financial support. anti-inflammatory (Lombardino & Wiseman, 1972), analgesic (Gupta et al, 2002), anti-cancer (Gupta et al, 1993), antibacterial (Zia-ur-Rehman et al, 2006) and endothelin receptor antagonists (Berryman et al, 1998), etc. In continuation of our research on the synthesis of biologically active benzothiazine derivatives (Ahmad et al, 2010), we herein report the synthesis and crystal structure of the title compound.…”