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Reaction of Benzyne with 1,2,5-Thiadiazoles and 2,1-Benzisothiazoles

1,2,5-Thiadiazoles react with benzyne to give 1,2-benzisothiazole derivatives. 3.4-Diphenyl-1,2,5-selenadiazole with benzyne likewise affords 3-phenyl-1,2-benzisoselenazole, contrary to a previous report.Some reactions of 3-(8-cyano-1-naphthyl)-1,2-benzisothiazole are described.The reaction of benzyne with 3-amino-2,1-benzisothiazole afforded N-phenylated products, including N-phenyl-anthranonitrile.

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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THERMAL FISSION OF HYDROXYLAMINE DERIVATIVES WITH NEIGHBOURING-GROUP-PARTICIPATION BY THIOETHER FUNCTIONS: PREPARATION OF 1,2-BENZISOTHIAZOLES

Some of the factors influencing the preparation of 1,2-benzisothiazoles from 2-(alkylthio)phenyl-substituted oximes are discussed.Good yields of 3-aryl-1,2-benzisothiazoles 4 may be obtained from readily available precursors.Reaction takes place under particularly mild conditions when a t-butylthio function is situated anti to the leaving group at oxime-nitrogen and S-N overlap is not restricted by ring-strain in the transition-state.The corresponding N-methyl-hydroxamic acid derivatives 2 give good yields of 2-methyl-1,2-benzisothiazol-3(2H)-one 13 only when a t-butylthio substituent is present, e.g. in 2f.The ethylthio- and i-propylthio-analogues 2d and 2e give the vinylthioethers 12, while the methylthio derivatives 2a-c undergo a novel rearrangement to “Pummerer” esters.The preparation of the polycyclic compounds fluoreno<9,9a,1-cd>-1,2 thiazole 7 and 2,2′-bi(2H-fluoreno<9,9a,1-de>-1,3-thiazine) 8 is described.

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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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Effect of power level on the microwave pyrolysis of tire powder

The pyrolytic performance of tire powder treated under different specific microwave powers (SMP), powers per 1?g sample, (9, 15, and 24?W/g) was investigated. The experimental results show that the pyrolysis level of tire powder was enhanced with increasing SMP. The maximum yields of liquid product (45%) and gas product (18.5%) were obtained at 15 and 24?W/g, respectively. In addition, the conversion rates of main organic elements transferred to three-phase products were calculated. All of the evolved gases were collected in successive gasbags, and 80% of the volumes were low-molecular-weight gases like H2, CH4 and C2H4; the fraction of gases generated increased with increasing SMP. The liquid products contained a large amount of aromatic hydrocarbons, and more limonene (nearly 10%) was produced in microwave pyrolysis than in conventional pyrolysis of tires. The proximate and ultimate analyses of the solid product showed a slight difference in composition as a function of SMP. Furthermore, there may be a competitive reaction between the sulfur release to the volatiles and sulfur fixation, forming ZnS; the amount of ZnS varied with SMP. The energy recovery was examined, which provides a useful measure of the energy efficiency of microwave pyrolysis process.

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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. I hope my blog about is helpful to your research. Application In Synthesis of Benzo[d]isothiazole

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Screening of yeasts isolated from Baijiu environments for 2-phenylethanol production and optimization of production conditions

2-Phenylethanol (2-PE) with a pleasant rose-like odor is a valuable aroma compound used in many fields. 2-PE production by yeast is considered a promising alternative to chemical synthesis and extraction from natural materials. In this report, the strain YF1702 produced a significantly higher level of 2-PE when compared with other strains isolated from Baijiu-producing environments. According to morphological properties, physiological and biochemical characteristics, and 26S rDNA sequence analysis, strain YF1702 was identified as Pichia kudriavzevii. The optimal fermentation conditions of YF1702 for producing 2-PE were obtained by single-factor experiments, Plackett?Burman design, steepest ascent design, and response surface methodology. The optimal inoculation conditions for strain YF1702 were 50?g/L glucose, 6.0?g/L yeast extract, 10.7?g/L L-Phe, and 32?g/L Tween-60. The optimal fermentation conditions were pH 2.3, 26?C, 210?rpm shaking, an inoculum size of 0.4% (v/v), and a loading volume of 25.5?mL/250?mL for 56?h. Under these optimal conditions 2-PE production by YF1702 was 5.09?g/L. This strain has the potential to increase the content of 2-PE in Baijiu production and enhance the aroma characteristics of Baijiu.

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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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INHIBITORS OF FACTOR XA WITH A NEUTRAL P1 SPECIFICITY GROUP

The present application describes inhibitors of factor Xa with a neutral P1 specificity group of formula I: STR1 or pharmaceutically acceptable salt forms thereof, wherein R and E may be groups such as methoxy and halo.

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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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Antihypertensive 1,2-benzisothiazole piperidines

There are described novel antihypertensive 1,2-benzisothiazole piperidines of the formula STR1 where X is hydrogen, halogen, loweralkoxy, loweralkyl, nitro, amino or trifluoromethyl; and R is STR2 R1 being loweralkyl, aryl, aralkyl, cycloalkylloweralkyl or a loweralkyl substituted with an amino, loweralkylamino or diloweralkylamino, and R2 being hydrogen, loweralkyl or aryl; antihypertensive compositions comprising said compounds or pharmaceutically acceptable acid addition salts thereof; and methods for synthesizing the same.

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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Article, the author is Omojokun, Olasunkanmi S. and a compound is mentioned, SDS of cas: 272-16-2, Benzo[d]isothiazole, introducing its new discovery. SDS of cas: 272-16-2

Alkaloid extracts from Bitter leaf (Vernonia amygdalina) and Black nightshade (Solanum nigrum) inhibit phosphodiesterase-5, arginase activities and oxidative stress in rats penile tissue

The erectogenic potential of alkaloids extracted from Bitter leaf (Vernonia amygdalina) and Black nightshade (Solanum nigrum) was investigated in this study. Fresh leaves obtained from Bitter leaf and Black night shade were air-dried, pulverized, and extracted for alkaloids. The inhibitory potential of the alkaloid extracts on arginase and phosphodiesterase-5 (PDE-5) activities in rats penile tissue was determined in vitro. The antioxidant properties were also evaluated and the constituent alkaloids quantified using GC-MS. The alkaloid extracts inhibited arginase (0?30.51?mug/ml) and PDE-5 (0?133.69?mug/ml) activities in a concentration-dependent pattern. Similarly, the alkaloid extracts inhibited Fe2+-induced lipid peroxidation in rats penile tissues, scavenged DPPH, OH, and NO radicals as a function of concentration. GC-MS characterization revealed over 20 alkaloid compounds. The inhibition of PDE-5-, arginase-, pro-oxidant-induced lipid peroxidative-, and free radicals-scavenging activities by the alkaloids is suggestive of putative mechanisms underlying their therapeutic use for managing erectile dysfunction in folklore medicine. Practical applications: Alkaloids extracted from Black nightshade (Solanum nigrum) and Bitter leaf (Vernonia amygdalina) were characterized and investigated by standard procedures for inhibitory action against key erectile dysfunction-linked enzymes and antioxidant activity. The alkaloids inhibited erectile dysfunction-linked enzymes (arginase and PDE-5) and showed considerable antioxidant activity in a concentration-dependent manner. In view of this, we suggest the application of these results in the development of erectile dysfunction drugs in the pharmaceutical industry, with probable minimal or no adverse effect.

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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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Quantitative analysis of the structure-activity relationship Of 1,2-Benzodiazole derivatives: DFT study

The relationship between the biological activity of compounds and their molecular structure is a predictor in rational drug design. Quantitative Structure Activity Relationships (QSAR) is one of the most important fields in chemometrics, they are based on the development of mathematical equations linking the chemical structure of a compound to its biological activity. QSAR is a molecular structure correlation process, or these derived properties with a particular type of biochemical activity. The properties of the compounds are determined by the density functional theory (DFT) method. The correspondence between the descriptors and the experimental activity uses multiple linear regressions (MLR). In this work, we have tested twenty-eight chemical compounds with the same molecule but with different functional groups using the approach Quantitative Structure Activity Relationships. Our results show that a good correlation between biological structure/activity (IC50). For a possible use of these molecules in the pharmaceutical field we studied their compliance with the rules of Lipinski.

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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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Effect of arbuscular mycorrhizal fungi inoculation on root traits and root volatile organic compound emissions of Sorghum bicolor

Volatile organic compounds (VOCs) emitted by plant roots have important functions that can influence the rhizospheric environment. The aim of this study was to examine the effects of arbuscular mycorrhizal (AM) fungi on the profile of root VOCs. Sorghum (Sorghum bicolor) plants were grown in pots inoculated with either Glomus mosseae or Glomus intraradices, which formed mycorrhiza with the roots. Control plants were grown in pots inoculated with sterile inoculum and did not form mycorrhiza. Forty-four VOCs were determined using headspace solid-phase microextraction (HS-SPME) and gas chromatography-mass spectrometry (GC-MS). Alkanes were the most abundant type of VOCs emitted by both mycorrhizal and non-mycorrhizal plants. Both the quantity and type of volatiles were dramatically altered by the presence of AM fungi, and these changes had species specificity. Compared with non-mycorrhizal plants, mycorrhizal plants emitted more alcohols, alkenes, ethers and acids but fewer linear-alkanes. The AM fungi also influenced the morphological traits of the host roots. The total root length and specific root length of mycorrhizal plants were significantly greater than those of non-mycorrhizal plants; however, both the incidence and length of root-hair were dramatically decreased. Our findings confirm that AM fungi can alter the profile of VOCs emitted by roots as well as the root morphology of sorghum plants, indicating that AM fungi have the potential to help plants adapt to and alter soil environments.

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Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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Aroma potential of Albillo wines and effect of skin-contact treatment

Free and glycosidically-bound aroma compounds were analysed in Albillo grape must, skin and wines, and the effects of different skin-contact treatments on aroma composition and wine sensory characteristics were evaluated. Musts and wines contained large amounts of C6 and benzene compounds. Must skin contact, at 18 C for 15 and 23 h, prompted a considerable increase in free and bound varietal compounds. Therefore, this technique, and the use of glycosidases are two methods recommended as a means for enhancing wine aroma. Skin-contact treatment intensified the fresh and fruity properties that were scored positively by wine tasters.

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com