- Novel palladium(II) and platinum(II) complexes of biocidal benzisothiazolinone (Bit); X-ray crystal structures of co-crystallised Bit/BitO and cis-Pd(en)(Bit-1H)2·H2O
-
Reaction of benzisothiazolinone (Bit), a well-known biocide, with the Pd(II) and Pt(II) am(m)ine precursors cis-[Pd(en)(H2O) 2](NO3)2 and cis-[Pt(NH3) 2(H2O)2](NO
- Griffith, Darren M.,Haughey, Aisleen,Chahal, Sunisha,Müller-Bunz, Helge,Marmion, Celine J.
-
-
Read Online
- Process Development of 1,2-Benzisothiazolin-3(2H)-one by Replacing of the Toxic Materials
-
1,2-Benzisothiazolin-3(2H)-one (2) was synthesized by 2,2′- dithiodibenzoic acid (1) with acetamide or urea in high yield via one-pot amidation-cyclization process.
- Jin, Chun Keun,Moon, Jung-Kyen,Lee, Woo Song,Nam, Keun Soo
-
-
Read Online
- Method for preparing 1, 2-benzisothiazolin-3-one through catalytic oxidation
-
The invention provides a method for preparing 1, 2-benzisothiazoline-3-one through catalytic oxidation, which comprises the following steps of: by taking a metal manganese salt or a manganese complex as a catalyst, carrying out oxidative cyclization react
- -
-
Paragraph 0025; 0029
(2021/08/06)
-
- Dimer impurity in ziprasidone hydrochloride raw material and preparation method thereof
-
The invention provides a dimer impurity in a ziprasidone hydrochloride raw material. The dimer impurity has a structure as shown in a formula 1. According to the invention, research and experiment are carried out from the mechanism direction, and it is believed that the compound 3-chloro-1, 2-benzothiazole can be subjected to self-condensation in the reaction process to generate the dimer impurity with the structure as shown in the formula 1. The impurity has extremely poor solubility and is slightly soluble in dimethyl sulfoxide or dichloromethane. The 3-chloro-1, 2-benzothiazole dimer impurity can be remained in the API without being controlled and removed, so the control of the dimer impurity in the preparation process of the 3-chloro-1, 2-benzothiazole and the anhydrous piperazine is particularly important. The invention further provides a preparation method for obtaining the high-purity ziprasidone hydrochloride dimer impurity, and the method is simple, high in controllability and mild in condition. The ziprasidone hydrochloride pharmaceutical composition can be used for ziprasidone hydrochloride process research and development, production, quality standard establishment and quality control links, and provides technical support for ziprasidone hydrochloride medication safety.
- -
-
Paragraph 0133-0136
(2021/06/09)
-
- Synthesis method of 1, 2-benzisothiazoline-3-ketone
-
The invention discloses a synthesis method of 1, 2-benzisothiazoline-3-ketone, which comprises the following steps: (1) adding 1, 2-dimercaptoethane and potassium carbonate at room temperature at one time, stirring, and slowly heating to obtain a mercapto
- -
-
Paragraph 0047-0054
(2021/04/10)
-
- Bioisosteric investigation of ebselen: Synthesis and in vitro characterization of 1,2-benzisothiazol-3(2H)-one derivatives as potent New Delhi metallo-β-lactamase inhibitors
-
Carbapenem-resistant Enterobacteriaceae (CRE) producing New Delhi metallo-β-lactamase (NDM-1) cause untreatable bacterial infections, posing a significant threat to human health. In the present study, by employing the concept of bioisosteric replacement of the selenium moiety of ebselen, we have designed, synthesized and characterized a small compound library of 2-substituted 1,2-benzisothiazol-3(2H)-one derivatives and related compounds for evaluating their cytotoxicity and synergistic activity in combination with meropenem against the E. coli Tg1 (NDM-1) strain. The most promising compound 3a demonstrated potent synergistic activity against a panel of clinically isolated NDM-1 positive CRE strains with FICI as low as 0.09. Moreover, its IC50 value and inhibition mechanism were also confirmed by using the enzyme inhibition assay and the ESI-MS analysis respectively. Importantly, compound 3a has acceptable toxicity and is not a PAINS. Because of its structural simplicity and potent synergistic activity in combination with meropenem, we propose that compound 3a may be a promising meropenem adjuvant and a new series of such compounds may worth further investigations.
- Jin, Wen Bin,Xu, Chen,Cheung, Qipeng,Gao, Wei,Zeng, Ping,Liu, Jun,Chan, Edward W.C.,Leung, Yun-Chung,Chan, Tak Hang,Wong, Kwok-Yin,Chen, Sheng,Chan, Kin-Fai
-
-
- Method for preparing benzo [d] isothiazoline-3 (2H)-ketone by catalytic molecular oxygen oxidation cyclization
-
The invention provides a method for preparing benzo [d] isothiazoline-3 (2H)-ketone by catalytic molecular oxygen oxidation cyclization. The method comprises the following steps: using a water-solubletransition metal phthalocyanine compound as a catalyst, reacting 2-mercaptobenzonitrile or 2, 2 '-dithiobenzonitrile in a water phase in an oxygen or air environment to generate benzo [d] isothiazoline-3 (2H)-ketone. The reaction is carried out in the water phase, and other organic solvents do not need to be added; the catalyst has high catalytic activity and high reaction efficiency; the preparation process is simple, the product selectivity is high, and byproducts are few; and the method is less in waste and environment-friendly and has a relatively wide industrial application prospect.
- -
-
Paragraph 0020-0024
(2020/05/09)
-
- Synthetic method 1-2 - benzisothiazol -3 -one compound (by machine translation)
-
The invention discloses a synthetic method of 1-2 - benzisothiazol -3 -one compound, and belongs to the field of chemical synthesis. 2 - 1-benzisothiazol 2 -one compounds are synthesized through acid chlorination, amidation and cyclization reaction by using the sulfenyl-substituted benzoic acid extracted from BIT process -3 - waste water as a starting raw material. The method disclosed by the invention has the advantages of mild reaction conditions, simple and convenient operation, strong practicability, less waste water, high product purity and the like, and is suitable for large-scale industrial production. The technical scheme provided by the invention is resource utilization and preparation 1 of wastewater extract produced in BIT production, and a feasible method is provided for the 2 -benzisothiazol -3 -one compound. (by machine translation)
- -
-
-
- Novel synthesis method of N-substituted benzisothiazoline-3-ketone derivative
-
The invention discloses a novel synthesis method of an N-substituted benzisothiazoline-3-ketone derivative. The preparation method comprises the following steps: by taking a dithiosalicylic acid derivative and sulfur as raw materials, introducing chlorine or bromine to obtain a halogenated thiobenzoyl halide derivative, then preferably dropwise adding a mixed solution of primary amine and tertiaryamine, and carrying out reaction and ring closing to obtain the N-substituted benzisothiazole-3-ketone. The method disclosed by the invention is simple in process, safe and controllable, and easy forindustrial large-scale production.
- -
-
-
- 1,2-BENZISOSELENAZOL-3(2H)-ONE AND 1,2-BENZISOTHIAZOL-3(2H)-ONE DERIVATIVES AS BETA-LACTAM ANTIBIOTIC ADJUVANTS
-
Provided herein are compositions and methods useful in the treatment of beta-lactam antibiotic resistant bacteria.
- -
-
Paragraph 0282-0285; 0331; 0332
(2019/10/04)
-
- Ebsulfur as a potent scaffold for inhibition and labelling of New Delhi metallo-β-lactamase-1 in vitro and in vivo
-
The superbug infection caused by New Delhi metallo-β-lactamase (NDM-1) has grown into an emerging threat, labelling and inhibition of NDM-1 has proven challenging due to its shuttling between pathogenic bacteria. Here, we report a potent covalent scaffold, ebsulfur, for targeting the protein in vitro and in vivo. Enzymatic kinetic study indicated that eighteen ebsulfurs gained except 1a–b and 1f inhibited NDM-1, exhibiting an IC50 value ranging of 0.16–9 μM, and 1g was found to be the best, dose- and time-dependent inhibitor with an IC50 of 0.16 μM. Also, these ebsulfurs effectively restored the antibacterial activity of cefazolin against E. coli expressing NDM-1, and the best effect was observed to be from 1g, 1i and 1n, resulting in an 256-fold reduction in MIC of the antibiotic at a dose of 16 μg/mL. The equilibrium dialysis study implied that the ebsulfur disrupted the coordination of one Zn(II) ion at active site of NDM-1. Labelling of NDM-1 using a constructed fluorescent ebsulfur Ebs-R suggested that the inhibitor covalently bound to the target through SDS-PAGE analysis in vitro. Also, labelling NDM-1 in living E. coli cells with Ebs-R by confocal microscopic imaging showed the real-time distribution change process of intracellular recombinant protein NDM-1. Moreover, the cytotoxicity of these ebsulfurs against L929 mouse fibroblastic cells was tested, and their capability to restore antibacterial activity of antibiotic against clinical strains E. coli EC08 producing NDM-1 was determined. The ebsulfur scaffold proposed here is valuable for development of the covalent irreversible inhibitors of NDM-1, and also for labelling the target in vitro and in vivo.
- Su, Jianpeng,Liu, Jiayun,Chen, Cheng,Zhang, Yuejuan,Yang, Kewu
-
supporting information
p. 192 - 201
(2018/12/02)
-
- A MBIT BIT and method of production
-
The invention discloses a method for coproducing BIT (1,2-benzisothiazoline-3-ketone) and MBIT (2-methyl-1,2-benzisothiazoline-3-ketone). The method comprises the following steps: 1) performing hydrolytic cyclization reaction on o-methylthiocyanophenyl serving as a raw material, water and chlorine, filtering and salifying the reaction liquid after the reaction to obtain a BIT salt aqueous solution, acidizing and filtering to obtain a BIT product, and absorbing, pressurizing and condensing a byproduct methane chloride generated in the reaction process to collect for later use; 2) adding the BIT salt aqueous solution obtained in the step 1) into a high-pressure kettle, adding the byproduct methane chloride obtained in the step 1), and performing temperature-increasing reaction to obtain a mixture containing the MBIT and a byproduct MOBIT (3-methoxyl-1,2-benzisothiazoline); 3) adding the mixture containing the MBIT and the byproduct MOBIT and obtained in the step 2) into the hydrolytic cyclization reaction in the step 1), performing demethylating reaction on the byproduct MOBIT to change into BIT and methane chloride, combining the MBIT with hydrogen chloride to form MBIT hydrochloride, and performing separation steps such as filtering and neutralizing on the reaction mixture to obtain BIT and MBIT products separately. The method has the advantages of reasonable process, energy saving, low pollution, capability of greatly reducing production cost and the like.
- -
-
Paragraph 0039; 0041; 0041
(2019/06/27)
-
- Continuous production method for 1,2-benzisothiazolin-3-one
-
The invention discloses a continuous production method for 1,2-benzoisothiazolin-3-one. According to the invention, o-chlorobenzonitrile is used as a starting material and subjected to a methylsulfation reaction and a chlorination reaction via a two-stage
- -
-
Paragraph 0019-0022
(2019/11/29)
-
- Pipeline type continuous production method of 3-isothiazolinone compound
-
The invention discloses a pipeline type continuous production method of a 3-isothiazolinone compound, which comprises the following steps: carrying out mixed reaction on a thioamide compound, a catalyst, a solvent and chlorine through a pipeline reactor system, and carrying out after-treatment after the reaction is completed to obtain the 3-isothiazolinone compound. According to the method, the defects of large occupied area, small productivity, low efficiency, high energy consumption and small safety coefficient caused by existing batch production of the 3-isothiazolinone compound are overcome; the invention provides a mode for continuously producing the 3-isothiazolinone compound, so that the reaction process is easy to control, energy consumption is reduced, the production efficiency and the safety coefficient of the production process are improved, and the process is an efficient and energy-saving safe production process.
- -
-
Paragraph 0021
(2019/12/02)
-
- Benzisothiazol-3-ones through a Metal-Free Intramolecular N–S Bond Formation
-
The highly efficient synthesis of benzoisothiazol-3-ones from thiobenzamides has been described with good functional group compatibility and excellent yields. This work represents the first example of selectfluor-promoted N–S bond formation processes. This method provides a facile approach to access various important bioactive benzoisothiazol-3-ones.
- Yang, Ke,Zhang, Hao,Niu, Ben,Tang, Tiandi,Ge, Haibo
-
p. 5520 - 5523
(2018/10/26)
-
- Thermolysis-Induced Two- or Multicomponent Tandem Reactions Involving Isocyanides and Sulfenic-Acid-Generating Sulfoxides: Access to Diverse Sulfur-Containing Functional Scaffolds
-
Direct reaction of isocyanides with some sulfenic-acid-generating sulfoxides led to the effective formation of the corresponding thiocarbamic acid S-esters in good to high yields. A multicomponent reaction involving isocyanide, sulfoxide, and a suitable nucleophile has also been developed, providing ready access to a diverse range of sulfur-containing compounds, including isothioureas, carbonimidothioic acid esters, and carboximidothioic acid esters.
- Wu, Shengfeng,Lei, Xiaofang,Fan, Erkang,Sun, Zhihua
-
supporting information
p. 522 - 525
(2018/02/10)
-
- Benzisothiazole compound and preparation method thereof and purpose of benzisothiazole compound for treating depression
-
The invention discloses a benzisothiazole compound and a preparation method thereof and a purpose of the benzisothiazole compound for treating depression. The benzisothiazole compound has a structureshown as a formula I. The research found that the compound in the formula I or its medicinal salt has the following good medicine properties of 5-HT1A acceptor excitement and 5-HT/NE reuptake inhibition effect, and has strong and rapid anti-depression effect in an animal depression model. The research result shows that the compound shown in the formula I or its medicinal salt can be used for treating depression. The invention provides an effective technical means for efficiently and rapidly treating the depression.
- -
-
Paragraph 0054; 0056; 0058; 0059
(2018/09/12)
-
- 1,2-benzisothiazolin-3-one synthesis method
-
The invention relates to a synthetic method of 1, 2-benzisothiazolin-3-one. According to the method, benzamide and sodium thiosulfate are allowed to react in the presence of carrier sodium thiosulfate and catalyst to generate the 1, 2-benzisothiazolin-3-one. The method has the advantages such that the cost is low, the steps are few, the yield is high and the environment friendliness is high.
- -
-
Paragraph 0031-0037
(2017/06/27)
-
- An efficient approach to construct benzisothiazol-3(2: H)-ones via copper-catalyzed consecutive reaction of 2-halobenzamides and carbon disulfide
-
An efficient copper-catalyzed reaction for the synthesis of benzisothiazol-3(2H)-ones has been developed, starting from easily available 2-halobenzamides and carbon disulfide, which gave the corresponding target products in 30-89% yield for 25 examples. The reaction proceeds via a consecutive process with S-C bond and S-N bond formation.
- Li, Ting,Yang, Lei,Ni, Kaidong,Shi, Zhenyu,Li, Fei,Chen, Dongyin
-
p. 6297 - 6303
(2016/07/11)
-
- SYNTHETIC METHOD FOR THE PREPARATION OF 1, 2-BENZISOTHIAZOLIN-3-ONE
-
The present invention relates to a method for producing a 1,2-benzisothiazolin-3-one compound (I) by reacting a 2-halobenzonitrile compound (II) with a thiol compound (III) to form an intermediate (IV) and subsequently reacting the intermediate (IV) with a halogenation agent in the presence of water to form a reaction mixture (RM), comprising the 1,2-benzisothiazolin-3-one compound (I) and a halide compound (V).
- -
-
Paragraph 0266; 0267
(2015/12/05)
-
- Synthetic method for the preparation of 1,2-Benzisothiazolin-3-one
-
The present invention relates to a method for producing a 1,2-benzisothiazolin-3-one compound (I) by reacting a 2-halobenzonitrile compound (II) with a thiol compound (III) to form an intermediate (IV) and subsequently reacting the intermediate (IV) with a halogenation agent in the presence of water to form a reaction mixture (RM), comprising the 1,2-benzisothiazolin-3-one compound (I) and a halide compound (V). R3-SH (III), R3_X1(V),
- -
-
Paragraph 0159; 0160; 0161
(2015/12/18)
-
- PROCESS FOR PREPARING 1,2-BENZOISOTHIAZOLIN-3-ONES
-
Sodium sulfide hydrate is at least partially dehydrated by heating with N-methyl 2-pyrrolidone. 2-Chlorobenzamide is added to the mixture which is heated further. The mixture is cooled and treated with aqueous hydrogen peroxide to give the sodium salt of 1,2-benzisothiazolin-3-one in good yield. Acidification if desired gives rise to the free 1,2-benzisothiazolin-3-one.
- -
-
Paragraph 0049
(2014/10/29)
-
- 1,2-BENZISOTHIAZOL-3-ONE COMPOUND PRODUCTION METHOD
-
The present invention provides a method for producing 1,2-benzisothiazol-3-one compounds by reacting a 2-(alkylthio)benzonitrile compound with a halogenating agent in the presence of water, the method being characterized in that the reaction proceeds while the halogenating agent and water are gradually and simultaneously added to a reaction system containing the 2-(alkylthio)benzonitrile compound. The invention allows the simple and economical production of highly pure 1,2-benzisothiazol-3-one compounds, which are useful as antimicrobial agents, antifungal agents, etc.
- -
-
Paragraph 0039; 0040; 0042; 0043
(2014/02/15)
-
- METHOD FOR PRODUCING 1,2-BENZISOTHIAZOL-3-ONE COMPOUND
-
The present invention provides a method for producing a 1,2-benzisothiazol-3-one compound by reacting a 2-(alkylthio)benzonitrile compound with a halogenating agent in the presence of water, wherein an alkyl halide that is generated as by-product is reacted with a sulfide to form an alkylthiol, which is converted into an alkali metal salt, and then the resulting alkali metal salt is reacted with a 2-halobenzonitrile compound to be converted into a 2-(alkylthio)benzonitrile compound and reused as a starting material for the production of a 1,2-benzisothiazol-3-one compound. By means of the present invention, it is possible to efficiently use the by-product that is generated during the production of a 1,2-benzisothiazol-3-one compound and economically produce a 1,2-benzisothiazol-3-one compound without placing a burden on the environment.
- -
-
Paragraph 0073; 0074
(2014/02/15)
-
- Preparation of benzisothiazolones from 2-bromobenzamides and sulfur under copper catalysis conditions
-
A convenient two-stage method has been developed for preparing benz[d]isothiazol-3(2H)-ones from 2-bromobenzamides and sulfur in a one-pot process under copper catalysis conditions. The method is suitable for the synthesis of N-aryl-, benzyl-, and alkyl-substituted benzisothiazolones. The yields of the benzisothiazolones depend on the nature of the starting amide and can reach 91%.
- Krasikova,Katkevics
-
p. 1684 - 1690
(2013/07/04)
-
- PROCESS FOR PREPARING 1,2-BENZOISOTHIAZOLINE-3-ONE
-
Sodium sulfide hydrate is at least partially dehydrated by heating with N-methyl 2-pyrrolidone. 2-chlorobenzamide is added to the mixture which is heated further. The mixture is cooled and treated with aqueous hydrogen peroxide to give the sodium salt of 1,2-benzoisothiazoline-3-one in good yield. Acidification if desired gives rise to the free 1,2-benzoisothiazoline-3-one.
- -
-
-
- Synthesis of 1,2-benzisothiazolin-3-ones by ring transformation of 1,3-benzoxathiin-4-one 1-oxides
-
1,2-Benzisothiazolin-3-ones were synthesized from 1,3-benzoxathiin-4-one 1-oxides by means of a nonhazardous and inexpensive method. The 1,3-benzoxathiin-4-one 1-oxides were prepared by oxidation of 1,3-benzoxathiin-4-ones with hydrogen peroxide in the presence of a catalyst. Attack of amines on the carbonyl groups of the 1,3-benzoxathiin-4-one 1-oxides and subsequent elimination of carbonyl compounds likely produced sulfenic acids, which then underwent ring closure to afford the 1,2-benzisothiazolin-3-ones.
- Shimizu, Masao,Shimazaki, Teruaki,Yoshida, Tetsuya,Ando, Wataru,Konakahara, Takeo
-
experimental part
p. 3932 - 3936
(2012/07/14)
-
- Concise approach to benzisothiazol-3(2 H)-one via copper-catalyzed tandem reaction of o -bromobenzamide and potassium thiocyanate in water
-
A concise approach to various benzisothiazol-3(2H)-one derivatives has been developed by copper-catalyzed the reaction of o-bromobenzamide derivatives with potassium thiocyanate (KSCN) in water. The reaction proceeds via a tandem reaction with S-C bond and S-N bond formation.
- Wang, Fei,Chen, Chao,Deng, Geng,Xi, Chanjuan
-
experimental part
p. 4148 - 4151
(2012/06/18)
-
- Crucial role of selenium in the virucidal activity of benzisoselenazol- 3(2h)-ones and related diselenides
-
Various N-substituted benzisoselenazol-3(2H)-ones and their non-seleniumcontaining analogues have been synthesized and tested against selected viruses (HHV-1, EMCV and VSV) to determine the extent to which selenium plays a role in antiviral activity. The data presented here show that the presence of selenium is crucial for the antiviral properties of benzisoselenazol-3(2H)-ones since their isostructural analogues having different groups but lacking selenium either did not show any antiviral activity or their activity was substantially lower. The open-chain analogues of benzisoselenazol- 3(2H)-ones-diselenides also exhibited high antiviral activity while selenides and disulfides were completely inactive towards model viruses.
- Pietka-Ottlik, Magdalena,Potaczek, Piotr,Piasecki, Egbert,Mlochowski, Jacek
-
p. 8214 - 8228
(2011/03/19)
-
- Immobilized 1,2-benzisothiazolin-3-one
-
The present invention provides novel antimicrobial immobilized 1,2-benzisothiazolin-3-one/zinc oxide (BIT/ZnO) complexes useful as antimicrobial agents because of their resistance to being leached from the substrate to which they are attached. The present invention is also directed to methods for preparing the BIT/ZnO complexes, to BIT/ZnO complexes prepared by the novel methods, to methods for using the BIT/ZnO complexes to inhibit microbial growth or reduce the level of bacteria on the surface of a substrate, and to substrates protected from microbial attack by being treated with the BIT/ZnO complexes. The present invention is further directed to compositions comprising 1,2-benzisothiazolin-3-one which has been immobilized with zinc oxide.
- -
-
Page/Page column 5
(2008/06/13)
-
- Urease inhibitors
-
A urease inhibitor and an anti-Helicobacter pylori agent, which contain, as an active ingredient, an isothiazole derivative represented by the general formula (1): wherein R1 represents a hydrogen atom or an amino group, R2 represents a hydrogen atom, a lower alkyl group, or an acetyl group, and X represents a carbon atom or a nitrogen atom. These drugs are effective to prevent and treat gastrointestinal diseases caused by urease of Helicobacter pylori, such as chronic gastritis and gastroduodenal ulcer.
- -
-
-
- Synthesis of 1,2-benzisothiazolin-3-one by transamination of sulfenamides
-
N-Substituted sulfenamoylbenzoates were synthesized by transamination of N-unsubstituted sulfenamoylbenzoates with amines. The reaction did not always proceed by simple amine exchange between the amines and ammonia on the sulfur atom of the sulfenamides. In reactions with aliphatic amines, the sulfenamides cyclized to form N-substituted 1,2-benzisothiazolin-3-ones. The synthesis of 1,2-benzisothiazolin-3-ones by intramolecular transamination was also investigated by S-amination of 2-mercaptobenzamides.
- Shimizu, Masao,Takeda, Ayanobu,Fukazawa, Hidenori,Abe, Yoshimoto,Shibuya, Isao
-
p. 1855 - 1864
(2007/10/03)
-
- Convenient synthesis of 1,2-benzisothiazol-3(2H)-ones by cyclization reaction of acyl azide
-
1,2-Benzisothiazol-3(2H)-one was synthesized by treatment of 2-mercaptobenzoic acid with diphenyl phosphoryl azide, followed by cyclization of the resulting acyl azide at low temperature, where Curtius rearrangement did not occur. 5-Amino-1,2-benzisothiazol-3(2H)-one was similarly synthesized in one pot from 4-mercaptoisophthalic acid.
- Chiyoda,Iida,Takatori,Kajiwara
-
p. 1427 - 1428
(2007/10/03)
-
- A facile synthesis of 1,2-benzisothiazolin-3-ones from thiosalicylates
-
Synthesis of 1,2-benzisothiazolin-3-ones by cyclization of 2- sulfenamoylbenzoates, which were prepared from amination of thiosalicylates by hydroxylamine-O-sulfonic acid, was examined. Although treatment of methyl 2-sulfenamoylbenzoate on heating gave unexpected 2-(2- methoxycarbonylphenylthio)-1,2-benzisothiazolin-3-one, the treatment with base at room temperature afforded 1,2-benzisothiazolin-3-one in a good yield.
- Shimizu, Masao,Kikumoto, Hisashi,Konakahara, Takeo,Gama, Yasuo,Shibuya, Isao
-
p. 3005 - 3012
(2007/10/03)
-
- Method for producing 1,2-benzisothiazol-3-ones
-
A method for producing a 1,2-benzisothiazol-3-one, having the steps of carrying out a reaction of a 2-(alkylthio)benzaldehyde with a hydroxylamine to give a 2-(alkylthio)benzaldehyde oxime and carrying out a reaction of the 2-(alkylthio)benzaldehyde oxime with a halogenating agent; and a method for producing a 1,2-benzisothiazol-3-one, having the steps of carrying out a reaction of a 2-halobenzonitrile with an alkanethiol in a heterogeneous solvent system in the presence of a base to give a 2-(alkylthio)benzonitrile and carrying out a reaction of the 2-(alkylthio)benzonitrile with an halogenating agent in the presence of water.
- -
-
-
- Reactions of 3H-1,2-benzodithiol-3-one 1-oxide with amines and anilines
-
Reaction of 3H-1,2-benzodithiol-3-one 1-oxide with primary amines or anilines provides reasonable yields (40-70%) of the corresponding 1,2-benzisothiazolin-3(2H)-ones. These reactions may have relevance to the biological chemistry of 1,2-dithiolan-3-one 1-oxides and also offer a new method for the preparation of certain 1,2-benzisothiazolin-3(2H)-ones.
- Kim, Woongki,Dannaldson, Jeffrey,Gates, Kent S.
-
p. 5337 - 5340
(2007/10/03)
-
- Method for producing alkylsulfinylbenzamides and 1,2-benzisothiazol-3-ones
-
A method for producing an alkylthiobenzamide by carrying out a reaction of a halobenzamide with an alkanethiol in the presence of a base in a heterogeneous solvent; a method for producing an alkylsulfinylbenzamide by carrying out a reaction of an alkylthi
- -
-
-
- Agrochemical compositions and methods employing hymexazol and 1,2-benzisothiazolin-3-one
-
A combination of 3-hydroxy-5-methylisoxazole with an antimicrobial agent has good agricultural fungicidal activity which lasts longer than 3-hydroxy-5-methylisoxazole alone. The dihydrate of the calcium salt of 3-hydroxy-5-methylisoxazole has advantages over the free 3-hydroxy-5-methylisoxazole, other salts and the anhydrous compound.
- -
-
-
- Palatable solid pesticidal compositions of ethylene and vinyl acetate copolymer
-
The invention comprises compositions in solid form of ethylene/vinyl acetate copolymer with an effective amount of bioactive agent, a protein/carbohydrate-lipid source, 0 to 20% of an edible oil and optionally an attractant, dye, preservative, adversive agent and biomarker and the use, thereof, to control pests.
- -
-
-
- Rearrangement de thienobenzothiepinones en thienoisothiazolinone et benzoisothiazolinone
-
Dans les conditions de la reaction de Schmidt les thienobenzothiepinones 1, 2 et 13 subissent un rearrangement respectivement en N-benzylthienoisothiazolin-3-one (5) et benzoisothiazolin-3-one (6).Un mecanisme de ce rearrangement est propose.
- Daich, Abdelali,Decroix, Bernard
-
p. 1881 - 1884
(2007/10/02)
-
- 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.
- Bryce, Martin R.,Dransfield, Trevor A.,Kandeel, Kamal A.,Vernon, John M.
-
p. 2141 - 2144
(2007/10/02)
-
- Preparation of 1,2-benzisothiazolones
-
1,2-Benzisothiazolones and their alkali metal salts are prepared by reacting 2,2'-dithiodibenzamides in the presence of oxygen or oxygen donors in an aqueous alkaline medium to which a water-soluble organic solvent may be added and, if desired, freeing th
- -
-
-
- ANALGESIC 1,2-BENZISOTHIAZOL-3-YLPIPERAZINE DERIVATIVES
-
A series of non-opiate analgesics of Formula I STR1 wherein R 1 is hydrogen, alkyl, aralkyl, or aryloxyalkyl; R 2 is alkyl or hydrogen; and R 3 and R 4 are independently selected from hydrogen, alkyl, acyloxy, alkoxy, alkylthio, halogen, hydroxyl, or trifluoromethyl; or a pharmaceutically acceptable acid addition salt.
- -
-
-
- Synthesis and Biological Evaluation of 1-(1,2-Benzisothiazol-3-yl)- and (1,2-Benzisoxazol-3-yl)piperazine Derivatives as Potential Antipsychotic Agents
-
Members of the series of title compounds were tested for potential antipsychotic activity in relevant receptor binding assays and behavioral screens.Structure-activity relationships within the series are discussed.Compound 24 (BMY 13859-1), a (1,2-benzisothiazol-3-yl)piperazine derivative, was selected for further study because of its potent and selective profile in primary CNS tests.It was active in the Sidman avoidance paradigm and blocked amphetamine-induced stereotyped behavior in dogs for up to 7 h.The compound's lack of typical neuroleptic-like effects in therat catalepsy test and its failure to produce dopamine receptor supersensitivity following chronic administration indicate that it should not cause the movement disorders commonly associated with antipsychotic therapy.Although 24 has potent affinity for dopaminergic binding sites, its even greater affinity for serotonin receptors suggests that a serotonergic component may be relevant to its atypical profile.Compound 24 is currently undergoing clinical evaluation in schizophrenic patients.
- Yevich, Joseph P.,New, James S.,Smith, David W.,Lobeck, Walter G.,Catt, John D.,et al.
-
p. 359 - 369
(2007/10/02)
-
- Photochemical Ring-expansion Reaction of 1,2-Benzisothiazolinones
-
The photochemical reaction of a series of 2-aryl-1,2-benzisothiazol-3(2H)-ones (1) under deaerated conditions was found to give dibenzothiazepin-11(10H)-ones (2).A mechanism through a biradical species is proposed for the photoreaction.When the photolysis of 1 was carried out in the presence of oxygen, 2-aryl-1,2-benzisothiazol-3(2H)-one-1-oxides (11) were formed together with compounds 2.
- Kamigata, Nobumasa,Hashimoto, Satoshi,Kobayashi, Michio,Nakanishi, Hiroshi
-
p. 3131 - 3136
(2007/10/02)
-
