- A method for preparing of mesotrione
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The invention provides a preparation method of mesotrione. The preparation method comprises is capable of preparing the target product from raw materials such as ortho-nitrotoluene, chlorosulfonic acid, sulfoxide chloride, sodium sulfite, chloroactic acid, 1,3-cyclohexanedione in the presence of a catalyst and acid-base. The preparation method is based on common chemical raw materials, the reaction flow of each step is implemented under conventional operation conditions, the amount of three wastes is low, the total yield is above 61%, the purity of the product is high, the purity of the coarse product of the mesotrione is greater than 98%, and the coarse product of the mesotrione can be further purified; as a result, the preparation method of mesotrione is applicable to large-scale industrial production.
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Paragraph 0052; 0053; 0054
(2017/02/09)
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- SULFONE COMPOUNDS AS 5-HT6 RECEPTOR LIGANDS
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The present invention relates to novel sulfone compounds as 5-HT6 receptor ligands of the formula (I), and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable
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Page/Page column 10
(2013/02/28)
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- SULFONE COMPOUNDS AS 5-HT6 RECEPTOR LIGANDS
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The present invention relates to novel sulfone compounds as 5-HT6 receptor ligands of the formula (I), and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable
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Page/Page column 27
(2011/08/03)
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- Syntheses, biological evaluation and QSAR study on antitumor activity of 1,5-N,N′-disubstituted-2-(substituted benzenesulphonyl) glutamamides
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We have reported [unpublished data] the synthesis and QSAR of 5-substituted-2-(substituted benzenesulphonyl) glutamines which have shown the importance of steric factor on the aliphatic chain. N-Phthalyl isoglutamine, having the substitution at position 1 of the glutamic acid moiety, is the metabolite of recently approved thalidomide for different types of tumors by US FDA. Based on these, 36 new 1,5-N,N′-disubstituted-2-(substituted benzenesulphonyl) glutamamides were synthesized, as tools for further elucidation of the structural requirements for antitumor activity. All the synthesized compounds were tested for antitumor activity against Ehrlich Ascites Carcinoma (EAC) in Swiss albino mice using tumor weight as inhibitory parameter. Quantitative structure-activity relationship (QSAR) studies of these analogues revealed that the electron donating groups on the phenyl ring are found to be mandatory for the activity which was also proved by the negative coefficient of indicator parameter I3, for NO2 group on the phenyl ring. Molecular volume (MV) and steric factor at R5 position also plays a role in ligand-receptor interactions.
- Srikanth,Debnath, Bikash,Jha, Tarun
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p. 1841 - 1854
(2007/10/03)
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- Synthesis, screening and quantitative structure-activity relationship (QSAR) studies of some glutamine analogues for possible anticancer activity
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We described the syntheses, biological activities and QSAR studies of 36 new 5-n-substituted-2-(substituted benzenesulphonyl) glutamines 6-41 with different substitutions. These compounds were designed as structural analogues of most reactive amino acid, 'glutamine' (GLN), especially in the tumor cells. They present the new basic lateral chains at R5 position as well as different substitutions at 2′, 3′, 4′, and 5′ positions on the benzene ring. The synthesized compounds have been tested for antitumor activity against Ehrlich ascites carcinoma (EAC) in Swiss albino mice using percentage inhibition of tumor weight as inhibitory parameter. In order to elucidate the structural requirements for antitumor activity, quantitative structure-activity relationship (QSAR) studies have been performed using extra thermodynamic model of Hansch. QSAR equations showed that the electronic parameter (σ) on the aromatic ring system, steric parameter (Es) and to some extent Sterimol length of the substituent (L) on the aliphatic side chain correlate significantly with the antitumor activity. Resonance factor occupies the major electronic contribution on the aromatic ring system to the activity.
- Srikanth,Kumar,Ghosh, Balaram,Jha, Tarun
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p. 2119 - 2131
(2007/10/03)
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- Design and synthesis of potent and selective 5,6-fused heterocyclic thrombin inhibitors
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Thrombin, a serine protease, plays a central role in the initiation of thrombotic events. We report design, synthesis, and antithrombotic efficacy of XU817 (7), a nonpeptide 5-(amidino) indole thrombin inhibitor. Utilizing the co-crystal structure of XU817 bound in the active site of thrombin we were able to synthesize analogs with enhanced thrombin affinity.
- Dominguez, Celia,Duffy, Daniel E.,Han, Qi,Alexander, Richard S.,Galemmo Jr., Robert A.,Park, Jeongsook M.,Wong, Pancras C.,Amparo, Eugene C.,Knabb, Robert M.,Luettgen, Joseph,Wexler, Ruth R.
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p. 925 - 930
(2007/10/03)
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- Process for the preparation of aromatic sulfonyl chlorides
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A process for the preparation of aromatic sulfonyl chlorides of the formula I STR1 in which R1, R2 and R3 are identical or different and are hydrogen, fluorine, chlorine, bromine or iodine atoms, alkyl(C1 -C4), acetamido, nitro or carboxyl groups, or R1 and R2 together form an aromatic or heteroaromatic ring having 5 or 6 ring members, which can be substituted by fluorine, chlorine, bromine or iodine atoms, alkyl(C1 -C4), acetamido, nitro or carboxyl groups, by reaction of aromatic compounds of the formula II STR2 in which R1, R2 and R3 have the abovementioned meanings, with chlorosulfonic acid in excess or with chlorosulfonic acid or oleum and thionyl chloride, by reacting in the presence of sulfamic acid as a catalyst.
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- Ureylene phenylene anionic naphthalenesulfonic acids
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Novel ureylenebis[substituted-phenylenecarbonyl-(and sulfonyl)imino-substituted-phenylenesulfonylimino-naphthalenetrisulfonic acid hexaalkali metal salts], useful as inhibitors of the complement system of warm-blooded animals, the amino-substituted phenylenecarbonyl (and sulfonyl)imino-substituted-phenylenesulfonylimino-naphthalenetrisulfonic acid, trialkali metal salts, which are new intermediates for the preparation of the active ureylenes, and the process for their preparation.
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