6584-37-8Relevant academic research and scientific papers
Concise access to perimidines by palladium (II) complexes via acceptorless dehydrogenative coupling of alcohols
Clinton, Savarimuthu Selvan,Ma?ecki, Jan Grzegorz,Ramesh, Rengan
, (2022/05/10)
A facile protocol for the one-pot synthesis of 2,3-dihydro-1H-perimidines via dehydrogenative coupling of easily exploitable benzyl alcohols supported by new Pd(II) complexes has been reported. To accomplish the construction of perimidines, a new set of palladium(II) complexes [Pd(L)Cl (PPh3)] (1–3) encompassing biphenyl benzhydrazone ligands (L=L1–L3) has been reported as catalysts. Structural characterization by elemental analysis, FT-IR, NMR (1H and 13C), and mass spectral analyses confirmed the composition of synthesized complexes. The molecular structures complex 1 and complex 2 were unequivocally resolved using single-crystal X-ray diffraction. It reveals that the complex espoused distorted square-planar geometry around Pd(II) ion chelated by azomethine nitrogen and imidolate oxygen of biphenyl benzhydrazone ligands with labile chloride and a triphenylphosphine. Further, the selective synthesis of a broad range of functionalized perimidines has been accomplished via ADC of a variety of alcohols with 1,8-diamino naphthalene. The palladium complexes mediated catalytic synthesis offered good yields of perimidines up to 86% using only 0.5?mol% catalyst loading. A probable mechanism to the formation of perimidines was postulated from the results of control experimental investigations. The environmentally compassionate, greener ADC protocol progresses via the generation of aldehyde intermediate and releases only water and hydrogen gas.
A class of 2, 3 - dihydronaphth block pyrimidine analogs, its synthetic method, pharmaceutical composition and use thereof
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Paragraph 0185; 0187-0188; 0193, (2017/07/22)
The invention belongs to the technical field of medicines and relates to a 2,3-dihydronaphthalene-embedded m-diazabenzene analogue represented as the following general formula I and a preparation method thereof. The 2,3-dihydronaphthalene-embedded m-diazabenzene analogue has a function of inhibiting biological activities of different subtypes of a protein-tyrosine-phosphatase family (PTPases), can be used as a tool compound for researching a biological function correlation of the subtypes of the protein-tyrosine-phosphatase family (PTPases) in a cell signal transduction process, and provides a new approach for preventing and treating cancer, metabolic and immunological diseases, angiocardiopathy and neurological diseases.
1H-2,3-Dihydroperimidine derivatives: A new class of potent protein Tyrosine Phosphatase 1B inhibitors
Wang, Wen-Long,Yang, Dong-Lin,Gao, Li-Xin,Tang, Chun-Lan,Ma, Wei-Ping,Ye, Hui-Hua,Zhang, Si-Qi,Zhao, Ya-Nan,Xu, Hao-Jie,Hu, Zhao,Chen, Xia,Fan, Wen-Hua,Chen, Hai-Jun,Li, Jing-Ya,Nan, Fa-Jun,Li, Jia,Feng, Bainian
, p. 102 - 121 (2014/02/14)
A series of 1H-2,3-dihydroperimidine derivatives was designed, synthesized, and evaluated as a new class of inhibitors of protein tyrosine phosphatase 1B (PTP1B) with IC50 values in the micromolar range. Compounds 46 and 49 showed submicromolar inhibitory activity against PTP1B, and good selectivity (3.48-fold and 2.10-fold respectively) over T-cell protein tyrosine phosphatases (TCPTP). These results have provided novel lead compounds for the design of inhibitors of PTP1B as well as other PTPs.
