7766-38-3Relevant articles and documents
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Barker,S.A.,Somers,P.J.
, p. 287 - 296 (1970)
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Silyl Radical-Mediated Activation of Sulfamoyl Chlorides Enables Direct Access to Aliphatic Sulfonamides from Alkenes
Gouverneur, Véronique,Hell, Sandrine M.,Laudadio, Gabriele,Meyer, Claudio F.,Misale, Antonio,No?l, Timothy,Trabanco, Andrés A.,Willis, Michael C.
supporting information, p. 720 - 725 (2020/02/20)
Single electron reduction is more challenging for sulfamoyl chlorides than sulfonyl chlorides. However, sulfamoyl and sulfonyl chlorides can be easily activated by Cl-atom abstraction by a silyl radical with similar rates. This latter mode of activation was therefore selected to access aliphatic sulfonamides, applying a single-step hydrosulfamoylation using inexpensive olefins, tris(trimethylsilyl)silane, and photocatalyst Eosin Y. This late-stage functionalization protocol generates molecules as complex as sulfonamide-containing cyclobutyl-spirooxindoles for direct use in medicinal chemistry.
Design, synthesis and structure-activity relationship of diaryl-ureas with novel isoxazol[3,4-b]pyridine-3-amino-structure as multi-target inhibitors against receptor tyrosine kinase
Shi, Zhi-Hao,Liu, Feng-Tao,Tian, Hao-Zhong,Zhang, Yan-Min,Li, Nian-Guang,Lu, Tao
, p. 4735 - 4744 (2018/08/21)
Inspired by that the multi-target inhibitors against receptor tyrosine kinases (RTKs) have significantly improved the effect of clinical treatment for cancer, and based on the chemical structure of Linifanib (ABT-869, Abbott), two series of diaryl-ureas with novel isoxazol[3,4-b]pyridine-3-amino-structure were designed and synthesized as multi-target inhibitors against RTKs. The preliminary biological evaluation showed that several compounds exhibited comparable potency with Linifanib. Compound S21 was identified as the most potent inhibitor against Fms-like tyrosine kinase 3 (FLT-3), kinase insert domain containing receptor (KDR) and platelet-derived growth factor receptor β (PDGFR-β) with its IC50 values were 4 nM, 3 nM and 8 nM respectively, it also showed potent inhibitory activities against several cancer cells.
Synthesis of thermo- and photo-responsive polysiloxanes with tunable phase separation: Via aza-Michael addition
Feng, Kai,Li, Shusheng,Feng, Linglong,Feng, Shengyu
, p. 14498 - 14504 (2017/11/28)
Two kinds of thermo- and photo-dual-responsive polysiloxanes (DRPSs) with functional pendent groups, N-isopropyl amides and azobenzene (Azo) or salicylideneaniline (SA), were synthesized through a facile, effective, and catalyst-free aza-Michael addition of poly(aminopropylmethyl-siloxane) with N-isopropyl acrylamide and N-azobenzene acrylamide or N-salicylaldehyde acrylamide. The chemical structrures of DRPSs were systematically characterized using FT-IR, H NMR and UV-Vis spectroscopy. The as-prepared DRPSs with lower Azo or SA contents exhibited lower critical solution temperature (LCST)-type phase transition in water, which is reversible and can be controlled by temperature and UV light. The effects of Azo and SA contents on the responsive properties of DRPSs are examined in detail. The LCST decreased with the increasing Azo or SA content. Once the content of Azo or SA reached up to 5.7% or 8.2%, respectively, DRPSs could not be dissolved in water even in an ice bath. Higher values of the LCST were measured after irradiation of the polymer solutions due to the higher polarity of cis-Azo and keto-SA conformation, induced by irradiation. The differences in cloud points between the irradiated and the non-irradiated DRPS aqueous solutions increased up to 3.4 °C and 9.8 °C when combined with 3.8% Azo and 5.8% SA units, respectively.