14547-73-0Relevant articles and documents
Bis-picolinamide Ruthenium(III) Dihalide Complexes: Dichloride-to-Diiodide Exchange Generates Single trans Isomers with High Potency and Cancer Cell Selectivity
Basri, Aida M.,Lord, Rianne M.,Allison, Simon J.,Rodríguez-Bárzano, Andrea,Lucas, Stephanie J.,Janeway, Felix D.,Shepherd, Helena J.,Pask, Christopher M.,Phillips, Roger M.,McGowan, Patrick C.
, p. 6341 - 6356 (2017)
A library of new bis-picolinamide ruthenium(III) dihalide complexes of the type [RuX2L2] (X=Cl or I, L=picolinamide) have been synthesised and characterised. The complexes exhibit different picolinamide ligand binding modes, whereby one ligand is bound (N,N) and the other bound (N,O). Structural studies revealed a mixture of cis and trans isomers for the [RuCl2L2] complexes but upon a halide exchange reaction to yield [RuI2L2], only single trans isomers were detected. High cytotoxic activity against human cancer cell lines was observed, with the potencies of some complexes similar to or better than cisplatin. The conversion to [RuI2L2] substantially increased the activity towards cancer cell lines by more than twelvefold. The [RuI2L2] complexes displayed potent activity against the A2780cis (cisplatin-resistant human ovarian cancer) cell line, with a more than fourfold higher potency than cisplatin. Equitoxic activity was observed against normoxic and hypoxic cancer cells, which indicates the potential to eradicate both the hypoxic and aerobic fractions of solid tumours with similar efficiency. The activity of selected complexes against non-cancer ARPE-19 cells was also tested. The [RuI2L2] complexes were found to be more potent than the [RuCl2L2] analogues and also more selective towards cancer cells with a selectivity factor in excess of sevenfold.
Copper(ii) mediatedorthoC-H alkoxylation of aromatic amines using organic peroxides: efficient synthesis of hindered ethers
Sarkar, Souvik,Sahoo, Tapan,Sen, Chiranjit,Ghosh, Subhash Chandra
supporting information, p. 8949 - 8952 (2021/09/10)
Synthesis of hindered alkyl aryl ether derivatives (R-O-Ar) remains a huge challenge and highly desirable in organic and medicinal chemistry because extensive substitution on the ether bond prevents the undesired metabolic process and thus avoids rapid de
Method for selectively synthesizing halogenated arylamine through copper catalysis (by machine translation)
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Paragraph 0079-0082, (2020/12/30)
The method comprises the following steps: reacting a substrate with a halogenating reagent (III) in an organic solvent to obtain a catalyst. The reaction 0 - 80 °C is reacted at 0.5 - 6h under the action of an oxidizing agent, and after the reaction is finished, the reaction liquid is subjected to post-treatment to obtain the product halogenated aromatic amine compound. To the invention, direct synthesis of the halogenated aromatic amine compounds is achieved for the first time, and the problems that in the traditional method, the metal catalyst is expensive, the halogenated reagent toxicity is large, byproducts are large and the like are solved. At the same time, the product can take off the pyridine guide group through simple hydrolysis, and further functional groups can be combined into an aromatic heterocyclic compound. The method is simple and convenient to operate, mild in reaction conditions, high in selectivity, high in product yield and wide in substrate applicability, and is an efficient organic synthesis means. : Substrate: Halogenating agent: Product: (by machine translation)
