CAS: 22994-85-0; N-Benzyl-2-(2-Nitro-1H-Imidazol-1-yl)Acetamide

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Ethyl 2-(2-Nitro-1H-Imidazol-1-yl)Acetate 161490-37-5

📜Ethyl 2-(2-Nitro-1H-Imidazol-1-yl)Acetate 以79的收率获得苄哒唑
参考文献: Method Of Making Benznidazole[fr] Procédé De Production De Benznidazole
标题: Method Of Making Benznidazole[fr] Procédé De Production De Benznidazole
摘要:一种制备苯硝咪唑的方法,通过在搅拌反应物中使用r1-Oh溶剂,将2-硝基咪唑(化学式1)与卤代乙酸酯(化学式4)和碱反应,其中x选择自br,I和cl,而r1选择自甲基,乙基,异丙基,新丁基,异丁基和叔丁基,冷却反应物,向反应物中加入苄胺,搅拌反应物,向反应物中加入水,并在低温下搅拌2小时,过滤以获得苯硝咪唑蛋糕,将苯硝咪唑蛋糕溶解于混合溶剂溶液中,并结晶苯硝咪唑.一种使用低毒性醇溶剂(r1-Oh)进行单阶段反应生产苯硝咪唑的方法.一种通过将粗苯硝咪唑溶解于丙酮,甲醇和水的溶剂组合中,并结晶苯硝咪唑以获得高纯度苯硝咪唑的方法.

专利信息

专利号:US-11555047-B2
优先权日:2019-10-31
标题:One-step synthesis of phosphate-based inhibitors and applications thereof
发明人：D'ANTONIO EDWARD; PIERCE JOSHUA
权利人:UNIV SOUTH CAROLINA; UNIV NORTH CAROLINA STATE
摘要:One-step methods for forming phosphate-based enzyme inhibitors are disclosed. Methods include reacting o-phosphorylethanolamine with an acyl chloride at acidic conditions. Acyl chlorides can be derivatized. The phosphate-based enzyme inhibitors can inhibit enzymes of the pentose phosphate pathway including D-ribose-5-phosphate aldose-ketose isomerase enzymes such as T. cruzi ribose 5-phosphate isomerase type B and D-ribulose-5-phosphate 3-epimerase enzymes. Methods can be used in forming pharmaceutical compositions for use in treatment of disease caused by kinetoplastid parasites including T. cruzi, T. brucei, and Leishmania spp.

专利号:US-9220714-B2
优先权日:2006-03-16
标 题 :Nitrofuran compounds for the treatment of cancer and angiogenesis
发明人：SAULNIER SHOLLER GISELLE L; SWAMY NARASIMHA; KALKUNTE STAYAN; SINGH RAKESH K; BRARD LAURENT; KIM KYU KWANG
权利人:WOMEN AND INFANTS HOSPITAL OF RHODE ISLAND; UNIV BROWN; WOMEN AND INFANTS HOSPITAL RHODE ISLAND
摘要:The invention is directed to the synthesis and use of nitrofuran compounds, especially Nifurtimox, as medicaments to treat cancer, especially neuroblastoma, and to inhibit angiogenesis. The invention also provides compositions, unit dosage forms, and kits comprising the compounds.

专利号:US-9765036-B2
优先权日:2013-11-19
标题:Production method for producing N-benzyl-2-(2-nitro-1H-imidazol-1-yl) acetamide
发明人：HÃ NDAL VEGA ERLINDA; ARIAS RIVAS CARMEN ELENA; CUCHILLA DE MERLOS ANA KARINA
权利人:MINI DE EDUCACIÓN; MINI DE EDUCACION
摘要:The invention relates to the synthesis of a therapeutic agent which is effective against American trypanosomiasis (Chagas disease) caused by the protozoa Tripanosoma cruzi and transmitted by blood-sucking insects of the genera Triatoma or Rhodnius. This synthesis method is carried out in one step, in a solid state. It is a clean, simple, economical, rapid, easily implemented method, does not involve acid or base catalysts in the synthesis process, and is also environmentally friendly. It is a synthesis method for producing N-benzyl-2-(2-nitro-1-H-imidazol-1-yl)acetamide from the N-benzyl-2-hydroxyacetamide and 2-nitro-1H-imidazol reaction mixture, using microwave irradiation as an activation source in order to produce the N-benzyl-2-(2-nitro-1H-imidazol-1-yl)acetamide.

专利号:WO-2009026858-A1
优先权日:2007-08-28
标题 :Derivatives of acridinone as anti-parasitic, anti-fungal and anti-viral agents
发明人：PELLON CONDOM ROLANDO F; DOCAMPO PALACIOS MAITE L; PARDO ANDREU GILBERTO L; FERNANDEZ-CALIENES VALDES AYME; MENDIOLA MARTINEZ BARBARA JUDITH; ROJAS RIVERO LAZARA; D ACCORSO HAICCK NORMA BEATRIZ; FASCIO SILVA MIRTA LILIANA; DAMONTE LOTITO ELSA BEATRIZ; GARCIA CATTEBEKE CYBELE CARINA; SEPULVEDA SUCHECKI CLAUDIA SOLEDAD; MAZZUCCO GAVIEIRO MARIA BELEN; TALARICO SALINAS LAURA BEATRIZ; MAES LOUIS
权利人:CT DE QUIMICA FARMACEUTICA; PELLON CONDOM ROLANDO F; DOCAMPO PALACIOS MAITE L; PARDO ANDREU GILBERTO L; FERNANDEZ-CALIENES VALDES AYME; MENDIOLA MARTINEZ BARBARA JUDITH; ROJAS RIVERO LAZARA; D ACCORSO HAICCK NORMA BEATRIZ; FASCIO SILVA MIRTA LILIANA; DAMONTE LOTITO ELSA BEATRIZ; GARCIA CATTEBEKE CYBELE CARINA; SEPULVEDA SUCHECKI CLAUDIA SOLEDAD; MAZZUCCO GAVIEIRO MARIA BELEN; TALARICO SALINAS LAURA BEATRIZ; MAES LOUIS
摘要:The invention relates to the synthesis and evaluation of novel organic products as anti-parasitic, anti-fungal and anti-viral agents. More specifically, the invention relates to novel derivatives of 10-alyl- (I), 10-(3methyl-2-butenyl)- (II) and 10-(1,2propanodienyl)-9(10H)-acridinone (III) and a novel family of acridinones, 10-{[3-(6-hydroxy-2,2-dimethyltetrahydrofuro[2,3-d][1,3]dioxol-5-il)-4,5-dihydro-5-isoxazolyl] methyl}-9(10H) acridinone (IV) having the following formulas: wherein positions 1, 2, 3, 4, 5, 6, 7 and 8 of the acridinone ring are hydrogen atoms or halogens, groups consisting of hydroxyl, amino, nitro, alkyl with between 1 and 5 carbon atoms, trichloromethyl, trifluoromethyl, alkoxyl with between 1 and 6 carbon atoms (aryloxy substituted), aryl and alkylamino with between 1 and 6 carbon atoms (mono- and di-substituted), aryl and alkylamide with between 1 and 4 atoms of carbon, cyano, carboxyl, formyl, alkyl and arylsulfonic, mercapto substituted with alkylic chains having up to 5 carbon atoms, and sulfoxide aryl. Said derivatives have an activity against Plasmodium falciparum, Trypanosoma brucei and Trypanosoma cruzi protozoans, as well as Microsporum canis and strains of the Junin virus and Dengue.

专利号:US-7745456-B2
优先权日:2000-11-06
标题 :Synthesis and antimicrobial activity of novel dicationic “reversed amidinesâ€
发明人：BOYKIN DAVID W; TIDWELL RICHARD R; WILSON W DAVID; PERFECT JOHN R; STEPHENS CHAD E
权利人:UNIV NORTH CAROLINA; UNIV DUKE; UNIV GEORGIA STATE RES FOUND
摘要:The present invention relates to novel 2,5-bis{[alkyl (or aryl) imino] aminophenyl}furans and thiophenes of the general formula n nin which R 1 , R 2 , R 3 and R 4 are each independently selected from the group consisting of H, alkyl, alkoxy, halide, and alkylhalide groups; R 5 is H, alkyl or aryl; R 6 is H, alkyl, aryl, or NR 7 R 8 , in which R 7 and R 8 are each independently selected from the group consisting of H, alkyl and aryl; and X is O, S or NR 9 , in which R 9 is H or alkyl, and to the use of such compounds.

专利号:US-2021130381-A1
优先权日:2019-10-31
标 题 :One-Step Synthesis of Phosphate-Based Inhibitors and Applications Thereof