86071-21-8Relevant academic research and scientific papers
2,1,3-Benzothiadiazine derivatives: Synthesis and screening versus PDE4 enzyme
Tait, Annalisa,Luppi, Amedeo,Avallone, Rossella,Baraldi, Mario
, p. 653 - 663 (2007/10/03)
A series of N-1,3 disubstituted 2,1,3-benzothiadiazine derivatives (BTDs) were synthesized and evaluated for their inhibitory activity versus enzymatic isoform PDE4 extracted from U937 cell line. Some of the tested compounds showed a high PDE4 inhibitory activity at 100:μM and the IC50 value of the most interesting terms were evaluated. The structure-activity relationships of these compounds showed that the 3,5-di-tert-butyl-4-hydroxybenzyl moiety at N-1 position is important to obtain activity at micromolar level as previously reported. For the same compounds the antioxidant activity were evaluated highlighting 14 as the most significative one. The introduction of other bulky substituents in N-1 position is detrimental.
Process for the preparation of 3-isopropyl-benzo-2-thia-1,3-diazinone-(4)-2,2-dioxide
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, (2008/06/13)
The present invention relates to a process for the preparation of 3-isopropyl-benzo-2-thia-1,3-diazinone-(4)-2,2-dioxide which comprises preparing isopropyl sulfamoyl chloride in one step by reacting N,N'-diisopropyl-urea with phosphorus trichloride and chlorine in the presence of oleum and sulfuric acid and condensing the so obtained isopropyl sulfamoyl chloride at room temperature without any solvent in the presence of an excess of N,N-diethyl aniline with anthranylic acid methyl ester and subjecting the thus obtained N-isopropyl-N'-o-carbomethoxy-phenyl-sulfamide to cyclization in the presence of sodium methylate, extracting the obtained crude 3-isopropyl-benzo-2-thia-1,3-diazinone-(4)-2,2-dioxide with a mixture of methanol and water and after adding water to the aqueous-methanolic mixture and sedimenting the contaminations isolating a product of high purity.
Process for synthesizing N-isopropyl-N'-o-carbomethoxyphenylsulphamide
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, (2008/06/13)
In order to synthesize N-isopropyl-N'-o-carbomethoxyphenylsulphamide, sulphuric chlorohydrin is reacted with a pyridic base between -10° and 50° C., after which anthranilic acid methyl ester is firstly added at 0°-60° C., followed by isopropylamine at 0°-
