154258-82-9Relevant articles and documents
Synthesis of novel fluorophenylpyrazole-picolinamide derivatives and determination of their anticancer activity
Bj?rkling, Fredrik,Guguloth, Hanmanthu,Gundepaka, Prasad,Kankala, Shravankumar,Kesari, Chekrapani,Nerella, Srinivas,Rama, Koteshwar Rao,Thota, Niranjan
, p. 1 - 10 (2020/07/21)
A series of fluorophenylpyrazole-picolinamide derivatives were synthesized in high yields using a cross-coupling reaction catalyzed by in situ formed palladium-N-heterocyclic carbenes (Pd-NHCs). The synthesized novel derivatives were evaluated for in vitro anticancer activity against a panel of four human tumor cell lines, HeLa (cervical), A-549 (lung), MCF-7 (breast), and IMR-32 (neuroblastoma). Four compounds, 11c, 11e, 11j, and 11k, showed growth inhibition (low μM) comparable with the standard drug cisplatin, providing a preliminary structure–activity relationship for the series. The present procedure is operationally simple and works with a wide range of substrates and may thus be useful in further compound optimization.
Molybdenum-silver co-catalyzed cycloaddition of alkynes with: N -isocyanoiminotriphenylphosphorane (NIITP): An efficient strategy for the synthesis of monosubstituted pyrazoles
Mi, Pengbing,Lang, Jiajia,Lin, Shaojian
supporting information, p. 7986 - 7989 (2019/07/10)
A new molybdenum-silver co-catalyzed [3+2] cycloaddition of alkynes with N-isocyanoiminotriphenylphosphorane (NIITP) has been described. The NIITP serves as a non-toxic, facile "CNN" source. Over 30 substrates were successfully converted to the desired compounds in good to excellent yields.
Preparation method of pyrazole derivative (by machine translation)
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Paragraph 0066-0070, (2019/12/02)
The preparation method comprises the following steps: mixing an alkyne propyl alcohol derivative, a halogen source, an acid and a solvent, heating and reacting, and reacting to Meyer - Schuster generate the pyrazole derivative. Compared with the prior art, the preparation method disclosed by the invention has 91% the advantages of maximum yield, simple operation, mild conditions, high conversion rate, few byproducts and the like, and provides a brand-new synthetic method for construction of pyrazole compounds. (by machine translation)