99-30-9Relevant articles and documents
Activator free, expeditious and eco-friendly chlorination of activated arenes by N-chloro-N-(phenylsulfonyl)benzene sulfonamide (NCBSI)
Misal, Balu,Palav, Amey,Ganwir, Prerna,Chaturbhuj, Ganesh
supporting information, (2021/01/04)
N-Chloro-N-(phenylsulfonyl)benzene sulfonamide (NCBSI) has been explored for the first time as a chlorinating reagent for direct chlorination of various activated arenes and heterocycles without any activator. A comparative in-silico study was performed to determine the electrophilic character for NCBSI and commercially available N-chloro reagents to reveal the reactivity on a theoretical viewpoint. The reagent was prepared by an improved method avoiding the use of hazardous t-butyl hypochlorite. This reagent was proved to be very reactive compared to other N-chloro reagents. The precursor of the reagent N-(phenylsulfonyl)benzene sulfonamide was recovered from aqueous spent, which can be recycled to synthesize NCBSI. The eco-friendly protocol was equally applicable for the synthesis of industrially important chloroxylenol as an antibacterial agent.
Identification of Potent and Selective Inhibitors of Fat Mass Obesity-Associated Protein Using a Fragment-Merging Approach
Elboray, Elghareeb E.,Fujiwara, Yoshie,Itoh, Yukihiro,Kitao, Yuki,Kotoku, Masayuki,Mellini, Paolo,Oba, Makoto,Obika, Satoshi,Prakash, Muthuraj,Roy, Rohini,Singh, Ritesh,Suzuki, Takayoshi,Takada, Yuri,Takahashi, Yukari,Terao, Mitsuhiro,Wang, Dan Ohtan,Yamaguchi, Takao,Yamamoto, Chika,Yamashita, Yasunobu
supporting information, p. 15810 - 15824 (2021/11/18)
Fat mass obesity-associated protein (FTO) is a DNA/RNA demethylase involved in the epigenetic regulation of various genes and is considered a therapeutic target for obesity, cancer, and neurological disorders. Here, we aimed to design novel FTO-selective inhibitors by merging fragments of previously reported FTO inhibitors. Among the synthesized analogues, compound 11b, which merges key fragments of Hz (3) and MA (4), inhibited FTO selectively over alkylation repair homologue 5 (ALKBH5), another DNA/RNA demethylase. Treatment of acute monocytic leukemia NOMO-1 cells with a prodrug of 11b decreased the viability of acute monocytic leukemia cells, increased the level of the FTO substrate N6-methyladenosine in mRNA, and induced upregulation of MYC and downregulation of RARA, which are FTO target genes. Thus, Hz (3)/MA (4) hybrid analogues represent an entry into a new class of FTO-selective inhibitors.
Cyclic synthesis method of nitroaniline chloride
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Paragraph 0032; 0033; 0038; 0039, (2020/10/05)
The invention discloses a cyclic synthesis method of nitroaniline chloride. The cyclic synthesis method comprises the following steps: (1) mixing nitroaniline and sulfuric acid, and preheating to a chlorination reaction temperature; (2) respectively inputting the solution obtained in the step (1) and chlorine into a reactor to carry out a chlorination reaction, cooling the material obtained in thereaction to obtain a supersaturated solution, and crystallizing to separate out a supersaturated product namely nitroaniline chloride; and (3) carrying out solid-liquid separation on the material cooled in the step (2), carrying out flash evaporation on the obtained saturated nitroaniline chloride/sulfuric acid solution, recycling hydrogen chloride, and circulating hydrogen chloride to the step (1) to replace sulfuric acid for dissolving nitroaniline, thereby realizing cyclic synthesis of nitroaniline chloride. Product super-saturation precipitation and saturated solution circulation are realized, the proportion of raw materials in a reaction system is reduced, the reaction is promoted to enter a uniform liquid phase system, meanwhile, mother liquor can be recycled, and the purposes of high efficiency, controllability and comprehensive utilization of resources are achieved.