- High-efficiency low-pollution fenoxaprop-p-ethyl production process
-
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.
- -
-
-
- HMOX1 inducers
-
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.
- -
-
Page/Page column 63; 130
(2020/09/18)
-
- Herbicide composition containing metamifop and quinclorac
-
The invention discloses an herbicide composition containing metamifop and quinclorac. The herbicide composition comprises primary active ingredients and secondary active ingredients, wherein the primary active ingredients comprise the following components in parts by mass: 5-10 parts of metamifop and 10-20 parts of quinclorac; the secondary active ingredients are selected from the following components in parts by mass: 10-20 parts of cyhalofop-butyl, 3-8 parts of bispyribac-sodium, 1-6 parts of halosulfuron-methyl, 3-7 parts of pyrazosulfuron-ethyl and 6-10 parts of pyribenzoxim; and the secondary active ingredients refer to one of cyhalofop-butyl, bispyribac-sodium, halosulfuron-methyl, pyrazosulfuron-ethyl and pyribenzoxim. The invention relates to the technical field of herbicides. According to the herbicide composition containing metamifop and quinclorac disclosed by the invention, the problems such as herbicide resistant weed plants appearing, soil contamination, degradation of water, harm of non-weeds and the like are solved.
- -
-
Paragraph 0024; 0027; 0036; 0042; 0055
(2019/03/08)
-
- A high yield of 2, 6 - dichloro diozaiole preparation method
-
The invention provides a high yield of 2, 6 - dichlorobenzene and oxazole of the preparation method, in a solvent, 6 - chlorobenzene and wicked zuozuo alkone and phosphorus pentachloride, in presence of catalyst direct chlorination reaction, shall be 2, 6 - dichlorobenzene and oxazole product. Preparation method of this invention increases the elasticity of the operation, disposable feeding, obviously improves the yield, the reaction by-product ingredient is single, is only phosphoric acid and hydrochloric acid, its waste water is easy processing, can be made into phosphate fertilizer sale, reduce the production cost. And the preparation method is the atmospheric pressure and 60 - 70 °C of low temperature, its mild reaction conditions, which is easy to produce.
- -
-
Paragraph 0009; 0016-0023
(2019/06/07)
-
- Synthesis method of 2,6-dichlorobenzooxazole
-
The invention relates to the field of organic synthesis, and particularly relates to a synthesis method of 2,6-dichlorobenzooxazole. The synthesis method comprises the following steps: adding benzoxazolone and phosphorus oxychloride in a reaction container, carrying out dissolving by stirring, then adding a chlorination reagent, carrying out a chlorination reaction to obtain the 6-dichlorobenzooxazole, adding a certain amount of a catalyst, carrying out heating for reflux, carrying out a reaction for 6-12 hours, removing the solvent after the reaction is ended, and carrying out reduced pressure distillation to obtain the product 2,6-dichlorobenzooxazole. According to the preparation method of the 2,6-dichlorobenzooxazole, the route is short, the yield is high, operation is simple and convenient, three wastes (waste gas, waste water and industrial residue) generated in a reaction process are few, and the method is suitable for large-scale industrial production. In addition, the phosphorus oxychloride is used for replacing virulent phosgene, diphosgene, solid phosgene or phosphorus pentachloride, the safety coefficient during production is improved, and environment friendliness is achieved.
- -
-
Paragraph 0035; 0037; 0038; 0040; 0041; 0043; 0046; 0048
(2019/04/26)
-
- ANTIBIOTIC COMPOUNDS
-
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.
- -
-
-
- Method for preparing 2-chlorobenzoxazole and 2,6-dichlorobenzoxazole from o-aminophenol by taking solid triphosgene as chlorinating agent
-
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.
- -
-
Paragraph 0032-0034; 0037
(2018/12/05)
-
- Using solid light method preparation 2,6-dichlorobenzene and method for synthesis of the oxazole (by machine translation)
-
The invention discloses a synthesis method for preparing 2,6-dichlorobenzoxazole by photocuring, which comprises the following steps: mixing 2-sulfhydryl-6-chlorobenzoxazole and di(trichloromethyl)carbonate in a medium solvent, heating to 50 DEG C, slowly heating to 80-110 DEG C, and reacting for 0.5-3 hours while keeping the temperature of 80-110 DEG C; and after the reaction finishes, removing the solvent to obtain the 2,6-dichlorobenzoxazole. The invention does not use any catalyst, and only adopts staged heating and photocuring, so that the di(trichloromethyl)carbonate can almost completely react to obtain the end product by being slowly decomposed in the heating process. The invention has the advantage of mild reaction conditions and process, and does not pollute the end product 2,6-dichlorobenzoxazole. In the method, after desolventization, crystallization is directly carried out without any other after-treatment to obtain the 2,6-dichlorobenzoxazole of which the mass percentage is higher than 98% and the yield is higher than 98%.
- -
-
Paragraph 0020; 0037; 0038
(2017/03/08)
-
- Synthesis and insecticidal activity of novel dihalopropene derivatives containing benzoxazole moiety: A structure-activity relationship study
-
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
-
p. 120 - 123
(2013/11/06)
-
- DERIVATIVES OF HETEROARYLSULFONAMIDES, THEIR PREPARATION AND THEIR APPLICATION IN HUMAN THERAPY
-
The present invention concerns derivatives of heteroarylsulfonamides, notably as blockers of Kv potassium channels, and more particularly of channels Kv1.5, Kv4.3 or Kv11.1, their application in clinical therapy and their preparation methods. These compounds correspond to the following general formula (I): where R1 represents one or more substituents of the phenyl core X such as: hydrogen, halogen, trifluoromethyl, trifluoromethoxy, linear or branched C1-C4 alkyl, or linear or branched C1-C4 alkoxy, A represents oxygen or sulphur, B represents nitrogen when n=1 or 2 and D represents —C(═O)—, or B represents CH when n=0 and D represents —CH2O— or when n=1 and D represents —O—, R2 represents a hydrogen, a methyl, a fluorine or chlorine atom or a methoxy, HetAr represents a pyridyl or quinolyl group, possibly substituted by a group such as a linear or branched C1-C4 alkyl, a linear or branched C1-C4 alkoxy, a halogen, or a trifluoromethyl, and to their pharmaceutically acceptable salts.
- -
-
Paragraph 0089; 0090; 0091; 0092
(2013/07/19)
-
- Preparation, antibacterial evaluation and preliminary structure-activity relationship (SAR) study of benzothiazol- and benzoxazol-2-amine derivatives
-
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
-
p. 3044 - 3049
(2012/06/04)
-
- DERIVATIVES OF HETEROARYLSULFONAMIDES, THEIR PREPARATION AND THEIR APPLICATION IN HUMAN THERAPY
-
The present invention concerns derivatives of heteroarylsulfonamides, notably as blockers of Kv potassium channels, and more particularly of channels Kv1.5, Kv4.3 or Kv11.1, their application in clinical therapy and their preparation methods. These compounds correspond to the following general formula (I): where R1 represents one or more substituents of the phenyl core X such as: hydrogen, halogen, trifluoromethyl, trifluoromethoxy, linear or branched C1-C4 alkyl, or linear or branched C1-C4 alkoxy, A represents oxygen or sulphur, B represents nitrogen when n=1 or 2 and D represents ?C(=O)-, or B represents CH when n=0 and D represents ?CH2O? or when n=1 and D represents ?O?, R2 represents a hydrogen, a methyl, a fluorine or chlorine atom or a methoxy, HetAr represents a pyridyl or quinolyl group, possibly substituted by a group such as a linear or branched C1-C4 alkyl, a linear or branched C1-C4 alkoxy, a halogen, or a trifluoromethyl, and to their pharmaceutically acceptable salts.
- -
-
Page/Page column 20
(2012/06/15)
-
- Analgesic Compounds, Compositions, and Uses Thereof
-
The invention relates to compounds, compositions, and methods for diminishing pain in a subject in need thereof comprising administering the compounds and compositions herein described.
- -
-
Page/Page column 21
(2011/10/04)
-
- A mild and efficient one-pot synthesis of 2-aminated benzoxazoles and benzothiazoles
-
Previous syntheses of the biologically active 2-aminated benzoxazoles have relied on forcing thermal conditions to generate the products directly from the corresponding thiols. The resulting yields have ranged from moderate to poor. A mild and high-yielding alternative one-pot chlorination-amination procedure is described. Compounds with a variety of substitution patterns are reported and the methodology has been successfully extended to benzothiazoles. Palladium catalysis on suitably activated examples has been employed to generate the desired compounds of interest.
- Stewart, Gavin W.,Baxter, Carl A.,Cleator, Ed,Sheen, Faye J.
-
supporting information; experimental part
p. 3229 - 3231
(2009/08/15)
-
- Synthesis and evaluation of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 3: Heterocyclic P3
-
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.
-
p. 1975 - 1980
(2007/10/03)
-
- Method for producing chlorobenzoxazolene
-
The invention relates to a process for preparing chlorobenzoxazoles of the formula (I), in which R1, R2 and R4 are as defined in claim 1 andin case (a) R3=H, halogen, CN, NO2, C1-C5-alkyl, C1-C5-alkoxy, aryl or aryloxy, where each of the 4 lastmentioned radicals is unsubstituted or substituted, orin case (b) R3=chlorine,which comprises reacting benzoxazoles of the formula (II), in which R1, R2 and R4 are as defined in formula (I) and R3 in case (a) is as defined in formula (I) and R3 in case (b) is hydrogen,in the presence of an acidic catalyst with a chlorinating agent to give the monochlorination product (I) or in case (b) with an excess of the chlorinating agent to give the dichlorination product (I) in which R3=chlorine.
- -
-
-
- Process for the preparation of 2-chlorobenzoxazoles
-
The process for the preparation of 2-chlorobenzoxazoles of the formula STR1 wherein R1 and R2, independently of one another, are hydrogen or halogen comprising reacting a benzoxazolinone of the formula STR2 with a molar excess of phosphorus pentachloride.
- -
-
-
- Process for preparing 2-chlorobenzoxazoles
-
In the process for preparing 2-chlorobenzoxazoles of the formula STR1 wherein each of R1, R2, R3 and R4 is independently of one another, H, chloro or alkyl having 1 to 4 carbon atoms, which comprises reacting chlorine with 2-mercaptobenzoxazoles of the formula STR2 wherein the improvement comprises providing a melt of previously prepared 2-chloro-benzoxazole, adding the 2-mercaptobenzoxazole reactant to the 2-chlorobenzoxazole melt and simultaneously or subsequently passing chlorine into the melt, with the proviso that substituents R1 to R4 are identical in both the 2-chlorobenzoxazole melt and the 2-mercaptobenzoxazole reactant.
- -
-
-
- Process for the manufacture of 2,6-dichlorobenzoxazole and 2,6-dichlorobenzthiazole
-
A process for the manufacture of 2,6-dichlorobenzoxazole and 2,6-dichlorobenzthiazole by chlorinating K+ or Na+ salts of 6-chloro-2-mercaptobenzoxazole or of 6-chloro-2-mercaptobenzthiazole in halogenated hydrocarbons as suspending agents.
- -
-
-