98-60-2Relevant articles and documents
Facile synthesis of sulfonyl chlorides/bromides from sulfonyl hydrazides
Chen, Rongxiang,Xu, Shaohong,Shen, Fumin,Xu, Canran,Wang, Kaikai,Wang, Zhanyong,Liu, Lantao
, (2021/09/20)
A simple and rapid method for efficient synthesis of sulfonyl chlorides/bromides from sulfonyl hydrazide with NXS (X = Cl or Br) and late-stage conversion to several other functional groups was described. A variety of nucleophiles could be engaged in this transformation, thus permitting the synthesis of complex sulfonamides and sulfonates. In most cases, these reactions are highly selective, simple, and clean, affording products at excellent yields.
Preparation method of medical intermediate of parachlorobenzenesulfonyl chloride
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Page/Page column 4-6, (2019/03/08)
The invention discloses a preparation method of a medical intermediate of parachlorobenzenesulfonyl chloride. The preparation method specifically comprises the following steps: firstly, cyclodextrin is modified sequentially through maleic anhydride and tetradecyl trimethyl ammonium chloride, and the modified cyclodextrin is obtained; and then a reaction is conducted by adopting sodium 4-chlorobenzenesulfonate and thionyl chloride as raw materials and the modified cyclodextrin as a catalyst, and by being added with ammonium trifluoroacetate for assisting. The prepared medical intermediate of the parachlorobenzenesulfonyl chloride is high in yield and high in purity, the reacting conditions are easy to operate, the requirements for equipment are low, and control is easy.
Design, synthesis and biological evaluation of novel phenylsulfonylurea derivatives as PI3K/mTOR dual inhibitors
Zhao, Bingbing,Lei, Fei,Wang, Caolin,Zhang, Binliang,Yang, Zunhua,Li, Wei,Zhu, Wufu,Xu, Shan
, (2018/07/13)
Five series of novel phenylsulfonylurea derivatives, 19a–d, 20a–d, 21a–d, 22a–d and 23a–d, bearing 4-phenylaminoquinoline scaffold were designed, synthesized and their IC50 values against four cancer cell lines (HepG-2, A549, PC-3 and MCF-7) were evaluated. Most compounds showed moderate cytotoxicity activity against the cancer cell lines. Structure–activity relationships (SARs) and pharmacological results indicated that introduction of 4-aminoquinoline scaffold and phenylsulfonylurea scaffold were beneficial for anti-tumor activity. Moreover, para-methoxyl substitution of 4-anilino moiety and para-halogen substitution of phenylsulfonylurea have different impacts on different series of compounds. Furthermore, the micromolecule group substitution in the 6-position of the quinoline ring have a slight impact on the cellular activity of the target compounds.