- Electrophilic Activation of [1.1.1]Propellane for the Synthesis of Nitrogen-Substituted Bicyclo[1.1.1]pentanes
-
Strategies commonly used for the synthesis of functionalised bicyclo[1.1.1]pentanes (BCP) rely on the reaction of [1.1.1]propellane with anionic or radical intermediates. In contrast, electrophilic activation has remained a considerable challenge due to t
- A?ssa, Christophe,Duarte, Fernanda,Goundry, William R. F.,Livesley, Sarah,Morris, James A.,Robertson, Craig M.,Sterling, Alistair J.
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supporting information
(2021/11/30)
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- Reductive cyclization of o-phenylenediamine with CO2 and BH3NH3 to synthesize 1H-benzoimidazole derivatives
-
A simple and green protocol was developed for the reductive cyclization of o-phenylenediamine with CO2 and BH3NH3 to yield 1H-benzimidazole. The desired 1H-benzimidazole derivatives were produced under mild conditions. Mechanism investigation indicated that the coordination of o-phenylenediamine with the boron atom of BH3NH3 promoted the transfer of the formyl group to form a stable intermediate, which facilitated the intramolecular nucleophilic addition-elimination for the formation of target product. In this process, BH3NH3 served multifunctional roles, acting as a reducing agent and a formylation catalyst.
- Li, Xiao,Zhang, Junhua,Yang, Yue,Hong, Hailong,Han, Limin,Zhu, Ning
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supporting information
(2021/09/28)
-
- K2S as Sulfur Source and DMSO as Carbon Source for the Synthesis of 2-Unsubstituted Benzothiazoles
-
We describe a three-component reaction of o-iodoanilines with K2S and DMSO that provides 2-unsubstituted benzothiazoles in moderate to good isolated yields with good functional group tolerance. Electron-rich aromatic amines and o-phenylenediamines instead of o-iodoanilines provided 2-unsubstituted benzothiazoles and 2-unsubstituted benzimidazoles with and without K2S under similar conditions. Notably, DMSO plays three vital roles: carbon source, solvent, and oxidant.
- Deng, Guobo,Kuang, Daizhi,Liang, Yun,Yang, Yuan,Yu, Jiangxi,Zhang, Fuxing,Zhu, Xiaoming
-
supporting information
p. 3789 - 3793
(2020/06/04)
-
- Synthesis method of ammonium acetate mediated benzimidazole compound
-
The invention discloses a synthesis method of a benzimidazole compound mediated by ammonium acetate. The synthesis method comprises the following steps: adding an o-phenylenediamine compound, dimethylsulfoxide, an additive 1 and an additive 2 into a reaction tube, carrying out a stirring reaction at 130-150 DEG C, cooling the reaction product to room temperature after the reaction is finished, and carrying out separation and purification on the product to obtain the benzimidazole compound. The invention develops a method for synthesizing a benzimidazole compound under the mediation of ammonium acetate by taking DMSO as a carbon source and an oxidant and an o-phenylenediamine compound as a substrate under the condition of no metal catalyst. The synthesis method does not need a metal catalyst, and the required carbon source and oxidant have the characteristics of low toxicity, low price, easiness in obtaining, stable performance and the like. The method has the advantages of easiness inoperation, few steps, mild reaction conditions, better functional group tolerance and the like, and provides a new valuable way for synthesizing benzimidazole compounds.
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Paragraph 0057-0059
(2020/11/23)
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- METALLOENZYME INHIBITOR COMPOUNDS
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Provided are compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
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-
Page/Page column 45-46
(2020/07/25)
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- Visible-light-induced aerobic oxidative desulfurization of 2-mercaptobenzimidazolesviaa sulfinyl radical
-
A mild transition-metal-free non-toxic aerobic photoredox system was found to enable highly efficient desulfurization of 2-mercaptobenzimidazoles. This viable catalytic system includes Rose Bengal in a low catalyst loading as a photosensitizer and cheap, non-toxic NaCl in a catalytic amount as an additive, combined with an oxygen atmosphere. This protocol provides an important alternative access to a broad range of benzimidazole and deuterated benzimidazole products in generally high yields with good tolerance of various synthetically and pharmaceutically useful functionalities. The mechanistic studies reveal that both single electron transfer and energy transfer probably occur in the initial step and a sulfinyl radical intermediate is involved in the key desulfurization process.
- Deng, Guo-Jun,Fu, Mei,Huang, Huawen,Ji, Xiaochen,Li, Yongtong
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supporting information
p. 5594 - 5598
(2020/09/21)
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- Transition-metal and oxidant-free approach for the synthesis of diverse N-heterocycles by TMSCl activation of isocyanides
-
A highly efficient TMSCl-mediated addition of N-nucleophiles to isocyanides has been achieved. This transition-metal and oxidant-free strategy has been applied to the construction of various N-heterocyles such as quinazolinone, benzimidazole and benzothiazole derivatives by the use of distinct amino-based binucleophiles. The notable feature of this protocol includes its mild reaction condition, broad functional group tolerance and excellent yield. This journal is
- Chen, Fen-Er,Dong, Lin,Li, Hongyan,Liu, Jinxin,Luo, Liangliang,Xiao, You-Cai,Zhou, Yuan
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p. 29257 - 29262
(2020/10/02)
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- Facile access to: N-formyl imide as an N-formylating agent for the direct synthesis of N-formamides, benzimidazoles and quinazolinones
-
N-Formamide synthesis using N-formyl imide with primary and secondary amines with catalytic amounts of p-toluenesulfonic acid monohydrate (TsOH·H2O) is described. This reaction is performed in water without the use of surfactants. Moreover, N-formyl imide is efficiently synthesized using acylamidines with TsOH·H2O in water. In addition, N-formyl imide was successfully used as a carbonyl source in the synthesis of benzimidazole and quinazolinone derivatives. Notable features of N-formylation of amines by using N-formyl imide include operational simplicity, oxidant- A nd metal-free conditions, structurally diverse products, and easy applicability to gram-scale operation.
- Huang, Hsin-Yi,Liang, Chien-Fu,Lin, Xiu-Yi,Yen, Shih-Yao
-
supporting information
p. 5726 - 5733
(2020/08/21)
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- Supported Rhodium (Rh@PS) Catalyzed Benzimidazoles Synthesis Using Ethanol/Methanol as C2H3/CH Source
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An effective and stable polystyrene supported rhodium (Rh@PS) nano-catalyst has been synthesized by following reduction-deposition approach and applied for the selective benzimidazoles synthesis from 1,2-phenylenediamines and ethanol/methanol as C2H3/CH source. The ethanol/methanol in the presence of trace amounts of aerobic oxygen under Rh@PS catalysed condition, first participated in oxidation of alcohol followed by consecutive condensation, cyclization and hydrogen elimination reactions with 1,2-phenylenediamine gave the desired products in good yields. The Rh@PS catalyst in a single system performed both oxidation and reduction reactions in a selective/specific manner and applied for large substrate scope. Easy recovery, handling, stability, recyclability of the catalyst and less chance of metal contamination with the products are the added advantages of the process. (Figure presented.).
- Sharma, Saurabh,Sharma, Ajay,Yamini,Das, Pralay
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supporting information
p. 67 - 72
(2018/12/05)
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- Microwave use of amidine compounds in the aqueous phase benzoate synthesis of benzimidazole compounds method
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The invention discloses a microwave the use of amidine compounds in the aqueous phase benzoate synthesis of benzimidazole compounds, in the aqueous phase under microwave conditions adding benzoic amidine compound under alkaline condition [...] into benzimidazole reaction, invention an environment-friendly, the operation is simple, cheap and safe, efficient process for preparing benzimidazole method. Compared with the prior art, this method not only can be applied to a large number of functional groups, the productive rate is high, few by-products, and the operation is simple, safe, low cost, environmental protection; .
- -
-
Paragraph 0077
(2019/03/28)
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- In Situ Formation of Frustrated Lewis Pairs in a Water-Tolerant Metal-Organic Framework for the Transformation of CO2
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Frustrated Lewis pairs (FLPs) consist of sterically hindered Lewis acids and Lewis bases, which provide high catalytic activity towards non-metal-mediated activation of “inert” small molecules, including CO2 among others. One critical issue of homogeneous FLPs, however, is their instability upon recycling, leading to catalytic deactivation. Herein, we provide a solution to this issue by incorporating a bulky Lewis acid-functionalized ligand into a water-tolerant metal-organic framework (MOF), named SION-105, and employing Lewis basic diamine substrates for the in situ formation of FLPs within the MOF. Using CO2 as a C1-feedstock, this combination allows for the efficient transformation of a variety of diamine substrates into benzimidazoles. SION-105 can be easily recycled by washing with MeOH and reused multiple times without losing its identity and catalytic activity, highlighting the advantage of the MOF approach in FLP chemistry.
- Shyshkanov, Serhii,Nguyen, Tu N.,Ebrahim, Fatmah Mish,Stylianou, Kyriakos C.,Dyson, Paul J.
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supporting information
p. 5371 - 5375
(2019/03/17)
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- Catalytic synthesis of benzimidazoles and organic carbamates using a polymer supported zinc catalyst through CO2 fixation
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Utilization of carbon dioxide in chemical fixation for synthesis of fine chemicals like benzimidazoles, organic carbamates, etc. is in high demand in recent years as carbon dioxide is a cost effective, sustainable, and green renewable C1 source. In this article we present the design and synthesis of an organically modified polystyrene bound heterogeneous [PS-Zn(ii)-SALTETA] catalyst. The catalyst has been characterized thoroughly by Fourier transform infrared spectroscopy, atomic absorption spectroscopy, thermo gravimetric analysis, PXRD, SEM and EDAX studies. The catalyst was used for cyclization of o-phenylenediamines through insertion of carbon dioxide in order to produce benzimidazoles in the presence of dimethylamine borane (DMAB). The developed catalytic procedure is sustainable, economical and efficient owing to the utilization of ethanol/water as a biodegradable and environment friendly solvent system. Besides benzimidazole production the catalyst was also very active for manufacture of organic carbamates from anilines and n-butyl bromide under atmospheric CO2 pressure under solvent free conditions at room temperature and the catalytic protocol showed outstanding functional group tolerance. Moreover the catalyst is highly recyclable and reusable.
- Biswas, Imdadul Haque,Biswas, Surajit,Islam, Md Sarikul,Riyajuddin, Sk,Sarkar, Priyanka,Ghosh, Kaushik,Islam, Sk Manirul
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p. 14643 - 14652
(2019/09/30)
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- Cobalt-catalyzed synthesis of N-containing heterocycles: Via cyclization of ortho -substituted anilines with CO2/H2
-
The CO2-involved synthesis of chemicals is of great significance from the green and sustainable chemistry viewpoint. Herein, we report a non-noble metal catalytic system composed of CoF2, CsF and P(CH2CH2PPh2)3 (denoted as PP3) for the synthesis of N-containing heterocycles from ortho-substituted anilines and CO2/H2. Mechanism investigation indicates that [Co(PP3)H(CO2)]+ is a catalytically active intermediate under working conditions; and CsF plays important roles in activating ortho-substituted anilines via hydrogen bond interactions, thus promoting the formation of the final products. This catalytic system is highly efficient, and allows a wide scope of ortho-substituted anilines, together with excellent functional group tolerance, affording various N-containing heterocycles in good to excellent yields.
- Ke, Zhengang,Yu, Bo,Wang, Huan,Xiang, Junfeng,Han, Juanjuan,Wu, Yunyan,Liu, Zhenghui,Yang, Peng,Liu, Zhimin
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p. 1695 - 1701
(2019/04/10)
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- Ru@PsIL-Catalyzed Synthesis of N-Formamides and Benzimidazole by using Carbon Dioxide and Dimethylamine Borane
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This work reports the synthesis and characterization of ruthenium nanoparticles (Ru NPs) supported on polymeric ionic liquids (PILs). This catalyst shows high catalytic activity towards the N-formylation of amines and synthesis of benzimidazoles from 1,2-diamines and carbon dioxide (CO2) by reductive dehydrogenation of dimethylamine borane. This methodology shows excellent functional group tolerance with broad substrate scope towards the synthesis of N-formamides and benzimidazoles. Interestingly, this protocol also provides the tandem reduction of 2-nitroamines and CO2 to synthesize benzimidazoles. It was proposed that the ionic liquid phase of the polymer plays pivotal roles such as assisting the stabilization of nanoparticles electrostatically, providing an ionic environment, and controlling the easy access of the substrates/reagents to the active sites. The developed methodology utilizes CO2 as a C1 source and water/ethanol as a green solvent system. Additionally, the catalyst was found to be recyclable in nature and shows five consecutive recycling runs without significant loss in its activity.
- Saptal, Vitthal B.,Sasaki, Takehiko,Bhanage, Bhalchandra M.
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p. 2593 - 2600
(2018/04/30)
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- Synthesis of benzimidazoles from o-phenylenediamines and DMF derivatives in the presence of PhSiH3
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A simple approach to preparation of benzimidazoles from o-phenylenediamines and DMF derivatives, only employing PhSiH3 as promoter without any other additives, was reported. This route provided moderate to high yields with a broad substrate scope. A plausible mechanism for the reaction is proposed based on the spectroscopic characterization (e.g., HRMS and 1H NMR) of the reaction mixture.
- Zhu, Jianhua,Zhang, Zhenbei,Miao, Chengxia,Liu, Wei,Sun, Wei
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p. 3458 - 3462
(2017/05/31)
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- Atmospheric CO2 promoted synthesis of N-containing heterocycles over B(C6F5)3 catalyst
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B(C6F5)3 combined with atmospheric CO2 was found to be highly effective for the cyclization of ortho-substituted aniline derivatives with N,N-dimethylformamide (DMF), and a series of N-containing heterocycles including benzothiazoles, benzimidazoles, quinazolinone and benzoxazole were obtained in good to excellent yields.
- Gao, Xiang,Yu, Bo,Mei, Qingqing,Yang, Zhenzhen,Zhao, Yanfei,Zhang, Hongye,Hao, Leiduan,Liu, Zhimin
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p. 8282 - 8287
(2016/10/11)
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- CO2 as a C1 Source: B(C6F5)3-Catalyzed Cyclization of o-Phenylene-diamines To Construct Benzimidazoles in the Presence of Hydrosilane
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The catalytic construction of benzimidazoles using CO2 as a carbon source represents a facile and sustainable approach to obtaining these valuable compounds. Herein, we describe the B(C6F5)3-catalyzed synthesis of benzimidazoles via cyclization of o-phenylenediamines with CO2 and PhSiH3. This metal-free catalytic route achieves the desired products in high yield under convenient reaction conditions and is applicable to a broad substrate scope. A plausible mechanism for the reaction involving a frustrated Lewis pair pathway is proposed based on spectroscopic characterization (e.g., 13C NMR) of the reaction intermediates.
- Zhang, Zhenbei,Sun, Qiangsheng,Xia, Chungu,Sun, Wei
-
supporting information
p. 6316 - 6319
(2016/12/23)
-
- Supercritical methanol as solvent and carbon source in the catalytic conversion of 1,2-diaminobenzenes and 2-nitroanilines to benzimidazoles
-
Benzimidazoles and N-methylbenzimidazoles were synthesized by simply heating 1,2-diaminobenzenes in supercritical methanol over copper-doped porous metal oxides. These catalysts were derived from synthetic hydrotalcites that only contain earth-abundant starting materials. The carbon equivalents needed for the construction of the benzimidazole core originated from the solvent itself, which is known to undergo reforming to hydrogen and carbon monoxide through the formation of a formaldehyde intermediate. A variety of 1,2-diaminobenzenes were converted to the corresponding mixtures of benzimidazoles and N-methylated analogues in good yields. Interestingly, the more challenging, but readily available 2-nitroanilines, which require an additional reduction step prior to cyclization, could also be successfully converted to benzimidazoles in high selectivity. Furthermore, various other alcohols were applied besides methanol, to obtain 2-alkyl- and 1,2-dialkylbenzimidazoles. Preliminary mechanistic insights into the origins of N-alkylation as well as the reactivity of the nitro derivatives are discussed.
- Sun, Zhuohua,Bottari, Giovanni,Barta, Katalin
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p. 5172 - 5181
(2015/12/08)
-
- Method For Preparing Nitrogen Compounds
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The present invention relates to a method for preparing nitrogen compounds using carbon dioxide, and to the use of the method in the production of vitamins, pharmaceutical products, adhesives, acrylic fibres, synthetic leathers, pesticides, herbicides, antifungal agents and fertilisers. The invention also relates to a method for producing vitamins, pharmaceutical products, adhesives, acrylic fibres, synthetic leathers, pesticides, herbicides, antifungal agents and fertilisers, which includes a step of preparing nitrogen compounds using the method of the invention. The invention further relates to a method for preparing labelled nitrogen compounds using carbon dioxide and to the uses thereof.
- -
-
Paragraph 0192; 0193
(2015/06/03)
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- Deprotection of N-benzylbenzimidazoles and N-benzylimidazoles with triethylsilane and Pd/C
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The benzyl group is a protecting group for benzimidazoles and imidazoles that can survive acidic, basic, oxidizing, and reducing conditions. Deprotection, however, can require vigorous and potentially non-chemoselective methods. The triethylsilane–Pd/C reduction system is an exceptionally mild, convenient, and efficient method for deprotecting N-benzylbenzimidazoles that are unsubstituted at the 2- and 4-positions as well as suitably substituted N-benzylimidazoles.
- Graham, Thomas H.
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supporting information
p. 2688 - 2690
(2017/11/14)
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- Convenient two-step one-pot synthesis of benzimidazoles using 2-nitroanilines and thiourea dioxide
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A new convenient method for the conversion of 2-nitroanilines into benzimidazoles by two-step one-pot procedure is reported. The procedure involves the reduction of nitro group followed by the intramolecular cyclisation of the corresponding o-phenylenediamines utilising thiourea dioxide and sodium hydroxide at 70 °C in mixed solvents of H2O and EtOH (v/v, 3/1). The yields are good to excellent and the workup is simple.
- Pu, Shuai,Liang, Qiuxiang,Luo, Xi,Luo, Juan
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p. 118 - 120
(2014/03/21)
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- Ultrasound promoted expeditious, catalyst-free and solvent-free approach for the synthesis of N,N′-diarylsubstituted formamidines at room temperature
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An effortless and efficient protocol was developed for the synthesis of N,N′-diarylsubstituted formamidines under environment-friendly conditions. Ultrasonic energy was employed to obtain the desired products in excellent yields with high purity under solvent-free and catalyst-free conditions. Products were purified by the crystallization technique to avoid excess utilization of organic solvents.
- Dar, Bashir Ahmad,Ahmad, Syed Naseer,Wagay, Mohammad Arif,Hussain, Altaf,Ahmad, Nisar,Bhat, Khursheed Ahmad,Khuroo, Mohammad Akbar,Sharma, Meena,Singh, Baldev
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p. 4880 - 4884
(2013/09/02)
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- Completely N1-selective palladium-catalyzed arylation of unsymmetric imidazoles: Application to the synthesis of nilotinib
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The completely N1-selective Pd-catalyzed arylation of unsymmetric imidazoles with aryl halides and triflates is described. This study showed that imidazoles have a strong inhibitory effect on the in situ formation of the catalytically active Pd(0)-ligand complex. The efficacy of the N-arylation reaction was improved drastically by the use of a preactivated solution of Pd2(dba)3 and L1. From these findings, it is clear that while imidazoles can prevent binding of L1 to Pd, once the ligand is bound to the metal, these heterocycles do not displace it. The utility of the present catalytic system was demonstrated by the regioselective synthesis of the clinically important tyrosine kinase inhibitor nilotinib.
- Ueda, Satoshi,Su, Mingjuan,Buchwald, Stephen L.
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supporting information; experimental part
p. 700 - 706
(2012/03/07)
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- Lewis acid catalyst free synthesis of benzimidazoles and formamidines in 1,1,1,3,3,3-hexafluoro-2-propanol
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A simple, inexpensive, environmentally friendly and efficient route for the synthesis of benzimidazole and formamidine derivatives by the reaction of O-phenylenediamines or amines with orthoesters using hexafluoroisopropanol as a solvent/catalyst is described.
- Khaksar, Samad,Heydari, Akbar,Tajbakhsh, Mahmood,Vahdat, Seyed Mohammad
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experimental part
p. 1377 - 1381
(2011/02/22)
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- HYDRAZONE COMPOUNDS AND THEIR USE
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The present invention relates to hydrazone compounds of Formula I: (I) and pharmaceutically acceptable salts and stereoisomers thereof, wherein R1, R2, R3, R4, L1, and L2 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I as inhibitors of TRPM5 protein.
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Page/Page column 113
(2010/12/17)
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- A mild, efficient and one-pot synthesis of 2-substituted benzimidazoles by ZrOCl2. 8H2O catalyzed ring closure reaction
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A mild, efficient and one-pot synthesis of an array of 2-substituted benzimidazoles from an appropriate o-phenylenediamine and orthoesters such as orthoformate, orthoacetate and orthovalerate using ZrOCl2-8H 2O, at room temperature and under microwave irradiation is described. Ecofriendly, solvent-free methodology has been employed under microwave condition. Compared with the conventional method, microwave irradiation method has the advantages of excellent yields (81-93%) and shorter reaction time (5-10 min).
- Sanjeeva Reddy,Nagaraj
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experimental part
p. 1154 - 1159
(2009/04/11)
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- A highly effective sulfamic acid/methanol catalytic system for the synthesis of benzimidazole derivatives at room temperature
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Sulfamic acid/methanol was found to be an efficient catalytic system for the synthesis of benzimidazole compounds through the condensation of o-phenylenediamine with orthoester in high yields at room temperature.
- Zhang, Zhan-Hui,Li, Tong-Shuang,Li, Jian-Jiong
-
-
- Synthesis of 2-substituted benzimidazoles by iodine-mediated condensation of orthoesters with 1,2-phenylenediamines
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(Chemical Equation Presented) Iodine was found to be an efficient catalyst for the synthesis of 2-substituted benzimidazoles by the condensation of orthoesters and 1,2-phenylenediamines in good to excellent yields under mild reaction conditions.
- Zhang, Zhan-Hui,Li, Jian-Jiong,Gao, Yuan-Zhe,Liu, Yu-Heng
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p. 1509 - 1512
(2008/09/18)
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- Heterocyclic compounds as inhibitors of factor VIIa
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The present invention relates generally to compounds that inhibit serine proteases. In particular it is directed to novel heterocyclic compounds, or a stereoisomer or pharmaceutically acceptable salt, solvate, or prodrug form thereof, which are useful as selective inhibitors of serine protease enzymes of the coagulation cascade; for example thrombin, factor VIIa, factor Xa, factor XIa, factor IXa, and/or plasma kallikrein. In particular, it relates to compounds that are factor VIIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of using the same.
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Page/Page column 79
(2008/06/13)
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- Synthesis of 2-alkyl-substituted benzimidazoles by thermal decomposition of 2-azidobenzenamines in the presence of an aldehyde
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2-Substituted benzimidazoles were prepared by reaction of 2-azidoaminobenzenes with aldehydes under thermal conditions. The reaction probably proceeds via a sequential imine formation, azide decomposition forming a nitrene, and electrocyclization. Copyright Taylor & Francis Group, LLC.
- Wallace, Jeffery M.,Soederberg, Bjoern C. G.,Hubbard, Jeremiah W.
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p. 3425 - 3439
(2007/10/03)
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- Diaminopropionic acid derivatives
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A compound of formula 1a which is useful for treating reperfusion injury, and salts, prodrugs, and related compounds.
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-
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- Indole- and benzimidazole-substituted imidazole and benzimidazole derivatives
-
Novel compounds are disclosed having the formula STR1 wherein X, R1, R2, R3, R4, and R5 are substituents. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, as antihypertensive agents.
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- Heterocyclic amines having central nervous system activity
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Tricyclic nitrogen containing compounds, having central nervous system activity of the following structural formula: STR1 and pharmaceutically acceptable salts thereof wherein R1, R2, and R3 are independently hydrogen, C1-6 alkyl, alkenyl, or alkynyl, C3-10 cycloalkyl, or R1 and R2 are joined to form a C3-7 cyclic amine which can contain additional heteroatoms; X is hydrogen, C1-6 alkyl halogen, hydroxy, alkoxy, cyano, carboxamide, carboxyl, or carboalkoxyl; A is SO2, N, CH, CH2, CHCH3, C=O, C=S, C-SCH3, C=NH, C-NH2, C-NHCH3, C--NHCOOCH3, or C--NHCN. B is CH2, CH, C=O, N, NH or N--CH3 ; n is 0 or 1; and D is CH, CH2, C=O, O, N, NH or N--CH3. These new compounds are suitable for treating schizophrenia, Parkinson's disease, anxiety, depression or as compounds for lowering blood pressure in animal or human hosts.
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- Indole and benzimidazole-substituted dihydropyrimidine derivatives
-
Novel compounds having the formula STR1 and its isomer STR2 wherein R1, R2, R3, R4, R5, R6, R7 and X are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, an antihypertensive agents.
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- ONE ATOM LYNCH PIN TRANSFORMATIONS OF GOLD'S REAGENT
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A series of o-phenylenediamines and o-aminophenols have been reacted with Gold's reagent to yield benzimidazoles and benzoxazoles, respectively.Additionally, o-hydroxyacetophenone and anthranilamide, when reacted with Gold's reagent, were found to produce chromone and 3H-quinazoline-4-one, respectively.These transformations represent the use of Gold's reagent as a one atom lynch pin.
- Gupton, John T.,Correia, Keith F.,Foster, Bruce S.
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p. 365 - 376
(2007/10/02)
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