- High-efficiency low-pollution fenoxaprop-p-ethyl production process
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The invention discloses a high-efficiency and low-pollution production process of fenoxaprop-p-ethyl. The production process comprises the following specific steps: (1) preparing fenoxaprop-p-ethyl; S1, preparing sulfydryl-6-chlorobenzoxazole; S2, preparing 2,6-dichlorobenzoxazole; and S3, synthesizing the fenoxaprop-p-ethyl. According to the fenoxaprop-p-ethyl, fenoxaprop-p-ethyl is finally synthesized through preparation of sulfydryl-6-chlorobenzoxazole and preparation of 2,6-dichlorobenzoxazole, the technology is simple, operation is convenient, efficiency is high, the speed is high, the production cost is saved, the income is increased, and filter residues generated in the production process can be safely treated through the technology; the waste gas enters a waste gas treatment facility for treatment and is discharged after reaching the standard; and the wastewater is desalted, removed salt is washed and dried by methanol to serve as a byproduct, and evaporated condensate water enters a factory sewage treatment station to be treated, so that the aim of protecting the environment is fulfilled, and the functions of high efficiency and low pollution are achieved.
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Paragraph 0032-0040; 0053-0062; 0076-0084
(2021/07/31)
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- HMOX1 inducers
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The present invention is related to compounds of structure (I) as heme oxygenase 1 (HMOX 1) inducers. The present invention is also related a method of controlling the activity or the amount, or both the activity and the amount, of heme-oxygenase 1 in a mammalian subject. The definitions of the variables are provided herein.
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Page/Page column 62-63; 130
(2020/09/18)
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- Synthesis method of 2-mercapto-6-chlorobenzoxazole
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The invention discloses a method for continuously synthesizing 2-mercapto-6-chlorobenzoxazole by a micro-channel reactor, and belongs to the technical field of organic synthesis processes. The methodcomprises the specific steps: performing ring opening on 6-chlorobenzoxazolone in a sodium hydroxide solution to obtain precursor salt, performing continuous sulfhydrylation cyclization reaction on the precursor salt and carbon disulfide in a micro-channel reactor, and performing acidification, centrifugation and drying to obtain a 2-mercapto-6-chlorobenzoxazole refined product. Compared with a traditional intermittent synthesis method of 2-mercapto-6-chlorobenzoxazole, the method has the advantages that the utilization rate of carbon disulfide is increased, the amount of three wastes is reduced, and particularly, safety accidents such as material flushing and unorganized emission of hydrogen sulfide are avoided. The method is simple to operate, high in product yield, good in quality and more beneficial to industrial production.
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Paragraph 0007; 0017-0022
(2020/07/28)
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- ANTIBIOTIC COMPOUNDS
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The present invention relates to antibiotic compounds of formula (I), to compositions containing these compounds and to methods of treating bacterial diseases and infections using the compounds. The compounds find application in the treatment of infection with, and diseases caused by, Gram-positive and/or Gram-negative bacteria, and in particular in the treatment of infection with, and diseases caused by, Neisseria gonorrhoeae.
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Page/Page column 67; 68; 81; 82; 182
(2018/03/25)
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- Method for preparing 2-chlorobenzoxazole and 2,6-dichlorobenzoxazole from o-aminophenol by taking solid triphosgene as chlorinating agent
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The invention provides a method for preparing 2-chlorobenzoxazole and 2,6-dichlorobenzoxazole from o-aminophenol by taking solid triphosgene as a chlorinating agent. The method comprises the followingsteps: step 1, respectively preparing 2-benzoxazolone and 2-mercapto benzoxazole by taking the o-aminophenol as a raw material; step 2, preparing the 2-chlorobenzoxazole by taking the 2-mercapto benzoxazole as a raw material and the solid triphosgene as the chlorinating agent; step 3, preparing 6-chlorobenzoxazolone by taking TCCA and the 2-benzoxazolone as raw materials; step 4, preparing 2-mercapto-6-chlorobenzoxazole; step 5, preparing the 2,6-dichlorobenzoxazole by taking the 2-mercapto-6-chlorobenzoxazole as a raw material and the solid triphosgene as the chlorinating agent. The method provided by the invention is a brand-new preparation method, which has the advantages of less corrosion to equipment, high yield, less reaction time, mild reaction conditions, less by-products and reduced environmental pollution.
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- AlCl3-Promoted Synthesis of 2-Mercapto Benzoheterocycles by Using Sodium Dimethyldithiocarbamate as Thiocarbonyl Surrogate
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A simple, expeditious and high-efficiency synthetic method for the AlCl3-mediated one-pot preparation of 2-mercapto benzoheterocycles (2-mercapto benzothiazoles, benzoxazoles and benzimidazoles) is described. By the treatment of a series of S, O and N heteroatoms containing bifunctional molecules with sodium dimethyldithiocarbamate in AlCl3, the desired benzoheterocycles are obtained smoothly. The protocol can also be applied on the synthesis of a series of thiazolidine-2-thiones, imidazolidine-2-thiones. This novel synthetic approach has advantages such as ligand-free, high efficiency, short reaction time, readily available starting materials and simple experimental procedures.
- Liu, Xing,Zhang, Shi-Bo,Dong, Zhi-Bing
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p. 5406 - 5411
(2018/10/20)
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- An environmentally benign and efficient synthesis of substituted benzothiazole-2-thiols, benzoxazole-2-thiols, and benzimidazoline-2-thiones in water
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An efficient and practical method for the one-step synthesis of benzothiazole-2-thiols, benzoxazole-2-thiols and benzimidazoline-2-thiones by cyclization of 2-aminothiophenols, 2-aminophenols, and 1,2-phenylenediamines with tetramethylthiuram disulfide (TMTD) in water was described. The features of this method include metal/ligand-free, excellent yield, short reaction time and broad substrate scope. The method provides a facile and convenient preparation of some potentially biologically active compounds.
- Liu, Xing,Liu, Min,Xu, Wan,Zeng, Meng-Tian,Zhu, Hui,Chang, Cai-Zhu,Dong, Zhi-Bing
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p. 5591 - 5598
(2017/12/06)
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- Selective synthesis of 2-aminobenzoxazoles and 2-mercaptobenzoxazoles by using o-aminophenols as starting material
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2-Aminobenzoxazoles and 2-mercaptobenzoxazoles were selectively synthesized by treating o-aminophenols with dithiocarbamates and tetramethylthiuram disulfide (TMTD), respectively. With the promotion of NaH/CuI, the reaction of o-aminophenols with dithioca
- Liu, Min,Zeng, Meng-Tian,Xu, Wan,Wu, Li,Dong, Zhi-Bing
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supporting information
p. 4352 - 4356
(2017/10/17)
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- 2-sulfydryl-6-chlorobenzoxazole synthesis method
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The invention relates to the field of chemical industry, and discloses a 2-sulfydryl-6-chlorobenzoxazole synthesis method. The method includes the step: (1) alkali hydrolysis: uniformly mixing 6-chlorobenzoxazolone and alkali liquor, increasing the temperature to range from 95 DEG C to 100 DEG C, performing thermal reaction to generate 2-sodium hydroxy-4-chlorobenzene sodium amino acid and reducing the temperature to range from 75 DEG C to 80 DEG C to obtain solution A; (2) sulfydryl synthesis: dripping carbon disulfide into the solution A, and performing thermal reaction at the temperature ranging from 75 DEG C to 80 DEG C after dripping to generate 2-sodium sulfydryl-6-chlorobenzoxazole and obtain solution B; (3) acidification: dripping the solution B into hydrochloric acid, performing reaction to generate 2-sulfydryl-6-chlorobenzoxazole, and performing pressure filtration and drying to obtain fine 2-sulfydryl-6-chlorobenzoxazole. Reaction system PH (potential of hydrogen) ranges from 4 to 5. Compared with the prior art, the synthesis method cannot generate a large amount of gas within a short time, punching is avoided, and safety and environmental protection accidents are avoided.
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- 2-Aminobenzoxazole ligands of the hepatitis C virus internal ribosome entry site
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2-Aminobenzoxazoles have been synthesized as ligands for the hepatitis C virus (HCV) internal ribosome entry site (IRES) RNA. The compounds were designed to explore the less basic benzoxazole system as a replacement for the core scaffold in previously discovered benzimidazole viral translation inhibitors. Structure-activity relationships in the target binding of substituted benzoxazole ligands were investigated.
- Rynearson, Kevin D.,Charrette, Brian,Gabriel, Christopher,Moreno, Jesus,Boerneke, Mark A.,Dibrov, Sergey M.,Hermann, Thomas
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supporting information
p. 3521 - 3525
(2014/07/22)
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- Synthesis and insecticidal activity of novel dihalopropene derivatives containing benzoxazole moiety: A structure-activity relationship study
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Ten dichloropropene derivatives containing benzoxazole moiety were synthesized and bioassayed in order to determine their in vivo insecticidal activity. The structures of obtained compounds were identified by 1H NMR, MS and elemental analyses. The bioassay results indicated that compound 2-(3-(2,6-dichloro-4-(3,3-dichloroallyloxy)phenoxy)propoxy)-5-(trifluoromethyl) benzo[d]oxazole (5i, R1 is trifluoromethyl, R2 is H and n is 3) had the optimal structure with best insecticidal activity against Spodoptera exigua (100%) at 1 mg/L concentration, highlighting the importance of trifluoromethyl group. The structure-activity relationship of the synthesized compounds was discussed as well.
- Guan, Aiying,Qin, Yukun,Wang, Junfeng,Li, Bin
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p. 120 - 123
(2013/11/06)
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- Preparation, antibacterial evaluation and preliminary structure-activity relationship (SAR) study of benzothiazol- and benzoxazol-2-amine derivatives
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In this study, a novel benzothiazol- and benzooxazol-2-amine scaffold with antibacterial activity was designed and synthesized. Preliminary structure-activity relationship analysis displayed that compound 8t with a 5,6-difluorosubstituted benzothiazole was found to be a potent inhibitor of Gram-positive pathogens, and exhibited some potential against drug-resistant bacteria and without cytotoxicity in therapeutic concentrations. In addition, molecular docking studies indicated that Staphylococcus aureus methionyl-tRNA synthetase might be the possible target of these compounds. Taken together, the present study provides an effective entry to the synthesis of a good lead for subsequent optimization and a new small molecule candidate drug for antibacterial therapeutics.
- Ouyang, Liang,Huang, Yuhui,Zhao, Yuwei,He, Gu,Xie, Yongmei,Liu, Jie,He, Jun,Liu, Bo,Wei, Yuquan
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supporting information; experimental part
p. 3044 - 3049
(2012/06/04)
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- An environmentally benign procedure for the synthesis of substituted 2-thiobenzothiazoles, 2-thiobenzoxazoles, 2-thiobenzimidazoles, and 1,3-oxazolopyridine-2-thiols
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An improved environmentally benign procedure for the synthesis of substituted 2-thio-benzothia(oxa)zoles, 2-thiobenzimidazoles, and 1,3-oxazolopyridine-2-thiols by cyclization of 2-aminophenols, 2-aminothiophenols, 1,2-phenylenediamines, or 2-amino-3-hydroxypyridines with potassium O-ethyldithiocarbonate in PEG 400 or glycerol under directed microwave irradiation is described. The method can be applied to the synthesis of a variety of derivatives. Springer-Verlag 2011.
- Deligeorgiev, Todor G.,Kaloyanova, Stefka S.,Lesev, Nedyalko Y.,Vaquero, Juan J.
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experimental part
p. 895 - 899
(2012/01/06)
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- DIAZEPANE COMPOUNDS WHICH MODULATE THE CB2 RECEPTOR
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Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
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Page/Page column 38
(2009/05/30)
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- TRIAZOLE DERIVATIVES HAVING ANTIFUNGAL ACTIVITY, METHOD FOR THE PREPARATION THEREOF, AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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A triazole derivative of formula 1 or a pharmaceutically acceptable salt, hydrate, solvate or isomer thereof is superior to the conventional antifungal drugs in antifungal activity against a wide spectrum of pathogenic fungi, and has advantageously low toxicity.
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Page/Page column 30
(2009/01/24)
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- NOVEL PIPERAZINES, PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE THEREOF
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Disclosed are novel piperazine derivatives that act as agonists of the α7 nAChR. Also disclosed are phannaceutical compositions, methods of treating inflammatory conditions, methods of treating CNS disorders, methods for inhibiting cytokine release from mammalian cells and methods for the preparation of the novel compounds.
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Page/Page column 79
(2008/06/13)
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- Synthesis and evaluation of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 3: Heterocyclic P3
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A series of Nα-2-benzoxazolyl-α-amino acid-(arylaminoethyl)amides were identified as potent, selective, and noncovalent inhibitors of cathepsin S. Structure-activity relationships including strategies for modulating the selectivities among cathepsins S, K, and L, and in vivo pharmacokinetics are discussed. A X-ray structure of compound 3 bound to the active site of cathepsin S is also reported.
- Tully, David C.,Liu, Hong,Alper, Phil B.,Chatterjee, Arnab K.,Epple, Robert,Roberts, Michael J.,Williams, Jennifer A.,Nguyen, Khanhlinh T.,Woodmansee, David H.,Tumanut, Christine,Li, Jun,Spraggon, Glen,Chang, Jonathan,Tuntland, Tove,Harris, Jennifer L.,Karanewsky, Donald S.
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p. 1975 - 1980
(2007/10/03)
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- Benzoxazoline and benzimidazoline derivatives as novel aldose reductase inhibitors, part 2: Lead optimization
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We designed novel aldose reductase inhibitors, benzoxazoline and benzimidazoline derivatives, based on lead evolution from spiroquinazolinones. In order to optimize in vivo activity in the lens, variously substituted derivatives were synthesized. The relationship between structure and in vitro activity was also analyzed by comparative molecular field analysis. The optimized compound exhibited high potency in the lens.
- Nakao, Kazuya,Asao, Masaaki,Shirai, Hiroki,Saito, Kiyoshi,Moriya, Tamon,Iwata, Hiroshi,Matsumoto, Mamoru,Matsuoka, Yuzo,Shimizu, Ryo
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p. 631 - 642
(2007/10/03)
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- Process for the preparation of 2-mercaptobenzoxazoles
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2-Mercaptobenzoxazoles of the formula STR1 wherein R is hydrogen or halogen and M is hydrogen or a metal atom, are prepared by reacting an ortho-aminophenol or metal salts thereof, with an alkali metal trithiocarbonate in aqueous solution.
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