120-66-1Relevant articles and documents
Selective Preparation. 38. A Convenient Preparation of 2-(Acylamino)biphenyls and N-Acetylaniline Derivatives Using the tert-Butyl Group as a Positional Protective Function
Tashiro, Masashi,Fukuda, Yasuhisa,Yamato, Takehiko
, p. 1927 - 1928 (1983)
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Late-Stage Diversification of Biarylphosphines through Rhodium(I)-Catalyzed C-H Bond Alkenylation with Internal Alkynes
Zhang, Zhuan,Cordier, Marie,Dixneuf, Pierre H.,Soulé, Jean-Fran?ois
, p. 5936 - 5940 (2020)
We report herein P(III)-directed C-H bond alkenylation of (dialkyl)- and (diaryl)biarylphosphines using internal alkynes. Chloride-free [Rh(OAc)(COD)]2 acts as a better catalyst than commercially available [RhCl(COD)]2. Conditions were developed to control the mono- and difunctionalization depending on the alkyne stoichiometry. One of these novel bisalkenylated (dialkyl)biarylphosphines was employed for the preparation of a palladium(II) complex, and some of these functionalized ligands outperformed their corresponding unfunctionalized phosphines in Pd-catalyzed amidation with sterically hindered aryl chlorides.
Ortho-Alkylation of Acetanilides Using Alkyl Halides and Palladium Acetate
Tremont, Samuel J.,Rahman, Hayat Ur
, p. 5759 - 5760 (1984)
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Sunlight-assisted decomposition of cephalexin by novel synthesized NiS-PPY-Fe3O4 nanophotocatalyst
Torki,Faghihian
, p. 49 - 59 (2017)
In this research, the catalytic performance of NiS and NiS immobilized into the matrix of magnetite polypyrrole core/shell (Fe3O4@PPY) for degradation of cephalexin was investigated. After characterization, by FTIR, TG, XRD, VSM, DRS, PL, Brunauer–Emmett–Teller (BET), TEM and SEM techniques, the photocatalysts were used for degradation of a pharmaceutical pollutant; cephalexin under UV and sunlight irradiations. The results indicated that application of PPY-Fe3O4 as the catalyst supports significantly enhanced the photocatalytic activity of NiS. The degradation efficiency obtained by NiS-PPY-Fe3O4 was higher than the value obtained by NiS alone. Moreover, by use of the support, a significant red shift was occurred on the band gap energy of NiS resulting higher degradation of the pollutant under sunlight irradiation. Paramagnetic nature of the NiS-PPY-Fe3O4 photocatlyst enabled effective separation of the used catalysts from the reaction solution with the aid of an external magnetic field and avoiding the tedious filtration or centrifugation. Upon regeneration, the photocatalyst retained most of its initial efficiency. Addition of H2O2 to the photocatalyst mixture had an enhancing effect on the cephalexin degradation. The photodegradation products were identified by GC–MS technique.
Method for synthesizing P-chloroO-toluidine
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Paragraph 0086-0087, (2021/10/05)
The invention discloses a method for synthesizing p-chloroo-toluidine, which comprises the following steps: synthesizing o-toluidine and a protective agent in an organic solvent to obtain an amino-protected intermediate. The amino protected intermediate is added into hydrochloric acid, an oxidant is added for chlorination reaction, and a chlorination product is obtained. The chlorinated product is removed and the amino protecting group is removed to give p-chloroo-toluidine. The method for synthesizing p-chloroo-toluidine provided by the invention is high in yield, simple to operate, less in three wastes, high in product content and good in quality, and can be suitable for industrial mass production.
Microwave-assisted synthesis of (Piperidin-1-yl)quinolin-3-yl) methylene)hydrazinecarbothioamides as potent inhibitors of cholinesterases: A biochemical and in silico approach
Athar, Muhammad Makshoof,Awan, Sana Javaid,Iftikhar, Kiran,Javid, Noman,Khan, Imtiaz,Munir, Rubina,Murtaza, Shahzad,Zaib, Sumera,Zia-Ur-rehman, Muhammad
, (2021/06/14)
Alzheimer’s disease (AD), a progressive neurodegenerative disorder, characterized by central cognitive dysfunction, memory loss, and intellectual decline poses a major public health problem affecting millions of people around the globe. Despite several clinically approved drugs and development of anti-Alzheimer’s heterocyclic structural leads, the treatment of AD requires safer hybrid therapeutics with characteristic structural and biochemical properties. In this endeavor, we herein report a microwave-assisted synthesis of a library of quinoline thiosemicarbazones endowed with a piperidine moiety, achieved via the condensation of 6/8-methyl-2-(piperidin-1-yl)quinoline3-carbaldehydes and (un)substituted thiosemicarbazides. The target N-heterocyclic products were isolated in excellent yields. The structures of all the synthesized compounds were fully established using readily available spectroscopic techniques (FTIR,1H-and13C-NMR). Anti-Alzheimer potential of the synthesized heterocyclic compounds was evaluated using acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. The in vitro biochemical assay results revealed several compounds as potent inhibitors of both enzymes. Among them, five compounds exhibited IC50 values less than 20 μM. N-(3-chlorophenyl)-2-((8-methyl-2-(piperidin-1-yl)quinolin-3-yl)methylene)hydrazine carbothioamide emerged as the most potent dual inhibitor of AChE and BChE with IC50 values of 9.68 and 11.59 μM, respectively. Various informative structure–activity relationship (SAR) analyses were also concluded indicating the critical role of substitution pattern on the inhibitory efficacy of the tested derivatives. In vitro results were further validated through molecular docking analysis where interactive behavior of the potent inhibitors within the active pocket of enzymes was established. Quinoline thiosemicarbazones were also tested for their cytotoxicity using MTT assay against HepG2 cells. Among the 26 novel compounds, there were five cytotoxical and 18 showed proliferative properties.
