CAS: 99-56-9; 4-Nitrobenzene-1,2-Diamine

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2,4-二硝基苯胺置于palladium On Activated Charcoal,氢气体系中,用 甲醇,乙酸乙酯 作为反应溶剂,化学反应生成 4-硝基邻苯二胺
参考文献:1-芳基-3-(4-甲氧基苄基)脲作为潜在不可逆的糖原合酶激酶3抑制剂:合成和生物学评估.
标题:1-芳基-3-(4-甲氧基苄基)脲作为潜在不可逆的糖原合酶激酶3抑制剂:合成和生物学评估.
摘要:糖原合酶激酶3(gsk-3)因其多因素参与阿尔茨海默氏病的发病机理而闻名.在这项研究中,通过将亲电子战斗部结合到环支架上,合成了拟议的cys199靶向gsk-3β共价抑制剂,合成了1-芳基-3-(4-甲氧基苄基)脲的苯并噻唑和苯并咪唑组.与参考抑制剂ar-A014418(1,Ic50 = 0.072)相比,腈取代的苯并咪唑基尿素2B(ic50 = 0.086+/-0.023 µm)和卤代甲基酮取代的苯并咪唑基尿素9B(ic50 = 0.13+/-0.060 µm)具有较高的gsk-3β抑制活性. +/-0.043).结果表明,对2B和9B作为gsk-3β的潜在共价抑制剂的进一步研究,因为靶向相互作用可能提供改善的激酶选择性.
DOI:10.1016/j.Bmcl.2019.04.049

专利信息

专利号:US-9951049-B2
优先权日:2014-05-15
标题 :Pyrazole linked benzimidazole conjugates and a process for preparation thereof
发明人：KAMAL AHMED; SHAIK ANVER BASHA; KUMAR GAJJELA BHARATH; REDDY VANGALA SANTHOSH
权利人:COUNCIL OF SCIENT & INDUSTRIAL RESEACH; COUNCIL SCIENT IND RES
摘要:Pyrazole linked benzimidazole conjugates and a method for synthesis of one or more compounds having a pyrazole linked benzimidazole conjugate, particularly pyrazole linked benzimidazole conjugates that are useful as potential antitumor agents against human cancer cell lines, such as leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, renal cancer, prostate cancer and breast cancer. The process comprises the step of oxidative cyclization of o-phenylenediamines and 3-phenyl-1H-pyrazole-5-carbaldehydes with sodium metabisulphite in ethanol/methanol solvent system at a desired temperature for a period of time to obtain the pyrazole linked benzimidazole conjugate.

专利号:US-2018317484-A1
优先权日:2017-05-07
标题:Composition for inhibiting synthesis of mycotoxin without affecting the growth of the fungi
发明人：MEHTA ALKA; BOGA RAMESHBABU; P DHANAMJAYULU
权利人:VIT UNIV; BogaR Laboratories
摘要:A composition for inhibiting the growth of mycotoxins without affecting the growth of fungi is provided. The mycotoxin is an Aflatoxin and the fungus is an Aspergillus . The anti-aflatoxin composition comprises benzimidazole derivatives of Formula, n n n n n n n n n n where the A is hydrogen or C1-C6 alkyl or C6-C14 aryl; B is C1-C10 alkyl or C6-C14 aryl or oxygen, sulfur, nitrogen containing heteroaryl; C and D are hydrogen or C1-C6 alkyl or C1-C6 alkoxyl or C6-C14 aryl; E is hydrogen or nitro or cyano or carboxyl or acetamidoxime or amidoxime or C1-C6 alkyl or C1-C6 alkoxyl or C6-C14 aryl or oxygen, sulfur, and nitrogen containing heteroaryl; F is hydrogen or C1-C6 alkyl or C1-C6 alkoxyl or C6-C14 aryl or oxygen, sulfur, and nitrogen containing heteroaryl, and mixture thereof with corresponding salts.

专利号:US-3935314-A
优先权日:1971-11-24
标题 :Anti-hypertensive compositions of benzimidazole derivatives
发明人：WATTS ERIC ALFRED
权利人:BEECHAM GROUP LTD
摘要:Antihypertensive pharmaceutical compositions comprising a compound of the formula (II) ##SPC1## n or pharmaceutically acceptable salts or solvates thereof wherein R 1 is nitrile or amidino; R 2 is hydrogen or lower hydrocarbon; R 3 , R 4 , R 5 and R 6 which may be the same or different, are each selected from hydrogen, halogen, nitro, trifluoromethyl, lower alkyl, lower acyl, hydroxyl, lower etherified hydroxyl or lower acylated hydroxyl; together with a pharmaceutically acceptable carrier. The compounds of formula (II) are also useful as intermediates in the synthesis of the corresponding 2-aminoimidazoline compounds.

专利号:WO-2015183518-A1
优先权日:2013-03-15
标 题:Synthesis of and curing additives for phthalonitriles
发明人：KELLER TEDDY M; LASKOSKI MATTHEW; SAAB ANDREW
权利人:US GOVERNMENT; KELLER TEDDY M; LASKOSKI MATTHEW; SAAB ANDREW
摘要:A method of: providing a solution of a dichloroaromatic compound having an electron- withdrawing group bound to each aromatic ring containing one of the chloride groups; a dihydroxyaromatic compound or anion thereof; an organic transition metal complex or a transition metal salt; a base; and a solvent; and heating the solution to a temperature at which the dichloroaromatic compound and the dihydroxyaromatic compound react to form a dimetallic salt of an aromatic ether oligomer. The molar ratio of the dihydroxyaromatic compound to the dichloroaromatic compound is greater than 2: 1. Water formed during the heating is concurrently distilled from the solution. A composition having a mixture of the below compounds having a mole ratio of at least 1:20. Ar 1 and Ar 2 are independently selected aromatic groups. A composition comprising phthalonitrile compounds that comprise at least 5 mol% of the first compound below.

专利号:US-9090661-B2
优先权日:2009-03-27
标 题:Inhibitors of hepatitis C virus replication
发明人：COBURN CRAIG A; MCCAULEY JOHN A; LUDMERER STEVEN W; LIU KUN; VACCA JOSEPH P; WU HAO; HU BIN; SOLL RICHARD; SUN FEI; WANG XINGHAI; YAN MAN; ZHANG CHENGREN; ZHENG MINGWEI; ZHONG BIN; ZHU JIAN
权利人:MERCK SHARP & DOHME
摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

专利号:US-7060818-B2
优先权日:2003-02-21
标题:Synthesis of macrocyclic tetraamido compounds and new metal insertion process
发明人：HORWITZ COLIN P; GHOSH ANINDYA
权利人:UNIV CARNEGIE MELLON
摘要:An improved method of synthesizing a macrocyclic tetraamido compound includes protecting the amino portion of an amino carboxylic acid to form a protected amino carboxylic acid; exposing the protected amino carboxylic acid to a first solvent, preferably a hydrocarbon solvent, such as toluene or 1,2-dichloroethane, dichloromethane, dibromomethane and 1,2-dibromoethane. The carboxylic acid portion of the protected amino carboxylic acid is then converted to an activated carboxylic acid by one of esterification or acid halide formation, to form a protected amino activated carboxylic acid derivative. The protected amino activated carboxylic acid derivative is reacted with a diamine in the presence of a second solvent, such as THF or ,2-dichloroethane, dichloromethane, dibromomethane and 1,2-dibromoethane, to form a protected diamide diamine intermediate. Following deprotection, the diamide diamine intermediate is reacted with an activated diacid, such as an activated malonate, oxalate or succinate derivative to form the macrocyclic tetraamido compound. The macrocyclic tetraamido compound may further be complexed with a transition metal.