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
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
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.