2634-33-5Relevant articles and documents
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
Griffith, Darren M.,Haughey, Aisleen,Chahal, Sunisha,Müller-Bunz, Helge,Marmion, Celine J.
, p. 2333 - 2337 (2010)
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
Process Development of 1,2-Benzisothiazolin-3(2H)-one by Replacing of the Toxic Materials
Jin, Chun Keun,Moon, Jung-Kyen,Lee, Woo Song,Nam, Keun Soo
, p. 1967 - 1968 (2003)
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.
Method for preparing 1, 2-benzisothiazolin-3-one through catalytic oxidation
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Paragraph 0026, (2021/08/06)
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
Dimer impurity in ziprasidone hydrochloride raw material and preparation method thereof
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Paragraph 0133-0136, (2021/06/09)
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.
Synthesis method of 1, 2-benzisothiazoline-3-ketone
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Paragraph 0047-0054, (2021/04/10)
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
Synthetic method 1-2 - benzisothiazol -3 -one compound (by machine translation)
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Paragraph 0047-0049, (2020/09/09)
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
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Paragraph 0041-0043, (2020/07/02)
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.
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
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
, (2020/04/30)
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.
Method for preparing benzo [d] isothiazoline-3 (2H)-ketone by catalytic molecular oxygen oxidation cyclization
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Paragraph 0020-0024, (2020/05/09)
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.
1,2-BENZISOSELENAZOL-3(2H)-ONE AND 1,2-BENZISOTHIAZOL-3(2H)-ONE DERIVATIVES AS BETA-LACTAM ANTIBIOTIC ADJUVANTS
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Paragraph 0282-0285; 0331; 0332, (2019/10/04)
Provided herein are compositions and methods useful in the treatment of beta-lactam antibiotic resistant bacteria.
