- Azosemide intermediate synthesizing method
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The invention discloses an azosemide intermediate synthesizing method. The method comprises the steps of performing tetrazole reaction to prepare a compound A: warming and enabling 4-chlorin-2-nitro benzonitrile and sodium azide to react under action of a catalyst and extracting reaction liquid by water to obtain reaction liquid of the compound A; directly performing hydrogenation reaction to prepare a compound B; performing chlorosulfonation reaction to prepare a compound C: slowly dropping qualified compound B and chlorosulfonic acid into cold water after temperature reaction and center control qualification, extracting through an organic solvent, standing for layering and decompressing, evaporating and drying the solvent in an organic phase mode to obtain a compound crude product C; performing ammonolysis reaction to prepare a compound D. Compared with the prior art, raw materials of the method disclosed by the invention are easy to obtain and low in cost; the method is low in cost, convenient to operate, suitable for industrialization and little in generated three wastes; furthermore, comprehensive utilization of waste can meet national industrial policy.
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Paragraph 0029; 0030; 0031
(2017/07/20)
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- FLT3 RECEPTOR ANTAGONISTS
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The invention pertains to novel FLT3receptor antagonists of general formula (1). The compounds are useful for the treatment or the prevention of pain disorders, cancer and autoimmune diseases.
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Page/Page column 51
(2016/03/29)
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- Synthesis of diverse azolo[c]quinazolines by palladium(II)- catalyzed aerobic oxidative insertion of isocyanides
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We report the palladium(II)-catalyzed aerobic oxidative coupling of isocyanides with various (2-aminophenyl)azoles using air as the stoichiometric oxidant. A diverse range of medicinally valuable azolo[c]quinazolines was obtained by this new approach.
- Vlaar, Tjostil,Bensch, Lisa,Kraakman, Jasper,Vande Velde, Christophe M. L.,Maes, Bert U. W.,Orru, Romano V. A.,Ruijter, Eelco
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supporting information
p. 1205 - 1209
(2014/05/06)
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- PYRIDOPYRIMIDINONE INHIBITORS OF PIM-1 AND/OR PIM-3
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Compounds of formula I, useful for inhibiting PIM-I and/or PIM-3: and pharmaceutically acceptable salts thereof, wherein Y, Z, R1, R3, Q, X and R4 are as defined above. Pharmaceutical compositions and methods of treating diseases and conditions, such as cancer, are also disclosed.
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Page/Page column 39
(2008/06/13)
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- Bioisosteric modifications of 2-arylureidobenzoic acids: Selective noncompetitive antagonists for the homomeric kainate receptor subtype GluR5
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2-Arylureidobenzoic acids (AUBAs) have recently been presented as the first series of selective noncompetitive GluR5 antagonists. In this paper we have modified the acidic moiety of the AUBAs by introducing different acidic and neutral groups, and similarly, we have replaced the urea linker of the AUBAs with other structurally related linkers. Replacing the acid with neutral substituents led to inactive compounds in all instances, showing that an acidic moiety is necessary for activity. Replacing the carboxylic moiety in 2a with a sulfonic acid (5c) or a tetrazole ring (5d) improved the potency at GluR5 receptors (compounds 5c and 5d showed IC50 values of 1.5 and 2.0 μM, respectively, compared to compound 2a with IC50 = 4.8 μM). Compound 5c did not show improved in vivo activity in the ATPA rigidity test compared to 2a, whereas compound 5d was 4 times more potent than 2a. All compounds wherein the urea linker had been replaced showed lower or no activity. The results described extend the knowledge of structure-activity relationships for the AUBAs, and compound 5d may prove to be a good candidate for studying GluR5 receptors in vitro and in vivo.
- Valgeirsson, Jon,Nielsen, Elsebet ?.,Peters, Dan,Mathiesen, Claus,Kristensen, Anders S.,Madsen, Ulf
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p. 6948 - 6957
(2007/10/03)
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- DIARYLUREA DERIVATIVES AND THEIR USE AS CHLORIDE CHANNEL BLOCKERS
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The present invention relates to novel diarylurea derivatives useful as chloride channel blockers. In other aspects the invention relates to the use of these compounds in a method for therapy, such as for the treatment of bone metabolic diseases, diseases responsive to modulation of the mast cell or basophil activity, diseases responsive to inhibition of angiogenesis, or sickle cell anaemia, and to pharmaceutical compositions comprising the compounds of the invention.
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- Novel synthesis of 5-substituted tetrazoles from nitriles
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A variety of 5-substituted tetrazoles were prepared through the respective reactions of sodium azide with corresponding nitriles in an aromatic solvent in the presence of an amine salt.
- Koguro, Kiyoto,Oga, Toshikazu,Mitsui, Sunao,Orita, Ryozo
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p. 910 - 914
(2007/10/03)
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