10552-10-0Relevant academic research and scientific papers
General Paradigm in Photoredox Nickel-Catalyzed Cross-Coupling Allows for Light-Free Access to Reactivity
Nocera, Daniel G.,Qin, Yangzhong,Sun, Rui
supporting information, p. 9527 - 9533 (2020/04/08)
Self-sustained NiI/III cycles are established as a potentially general paradigm in photoredox Ni-catalyzed carbon–heteroatom cross-coupling reactions through a strategy that allows us to recapitulate photoredox-like reactivity in the absence of light across a wide range of substrates in the amination, etherification, and esterification of aryl bromides, the latter of which has remained, hitherto, elusive under thermal Ni catalysis. Moreover, the accessibility of esterification in the absence of light is especially notable because previous mechanistic studies on this transformation under photoredox conditions have unanimously invoked energy-transfer-mediated pathways.
Synthesis and evaluation of some novel dibenzo[b,d]furan carboxylic acids as potential anti-diabetic agents
Lakshminarayana,Prasad, Y. Rajendra,Gharat, Laxmikant,Thomas, Abraham,Narayanan, Shridhar,Raghuram,Srinivasan,Gopalan, Balasubramanian
experimental part, p. 3709 - 3718 (2010/11/04)
A series of novel dibenzo[b,d]furan mono-carboxylic acid derivatives were synthesized, characterized and evaluated for their ability to inhibit Protein Tyrosine Phosphatase 1B (PTP1B) in vitro in order to use them as potential anti-diabetic agents. Structure-activity relationship study led to the identification of potent compound 5E which inhibited PTP1B with IC50 value of 82 ± 0.43 nM. Compound 5E was screened in vivo as drug candidate for anti-diabetic activity using rosiglitazone maleate as the standard. Compound 5E showed significant reduction in body weight, fed-state whole blood glucose (WBG), fasting WBG, plasma glucose and plasma cholesterol levels and non-significant reduction in fasting plasma triglyceride levels in ob/ob mice. A series of dibenzo[b,d]furan carboxylic acids were synthesized and evaluated for anti-diabetic activity. Compound 5E inhibited PTP1B with IC50 of 82 nM and reduced WBG and plasma glucose in ob/ob mice.
Solid phase synthesis of aryl amines
Willoughby, Christopher A.,Chapman, Kevin T.
, p. 7181 - 7184 (2007/10/03)
A method for the solid phase synthesis of aryl amines is reported. The method involves a palladium mediated coupling reaction between aryl bromides and amines. The products are isolated in high purity and good yields. This method should prove to be a useful tool for constructing combinatorial libraries containing the aryl amine moiety.
Studies of Tetriary Amine Oxides. 9. Thermal Rearrangement of 1-(4-Substituted-phenyl)piperidine N-Oxides to the Corresponding N-Hydroxylamines
Khuthier, Abdul-Hussain,Al-Mallah, Khawla Y.,Hanna, Salim Y.,Abdulla, Noor-Aldeen I.
, p. 1710 - 1713 (2007/10/02)
(4-Substituted - phenyl)piperidine N-oxides undergo a thermal rearrangement to O-arylhydroxylamines.Electron withdrawing substituents are essential for the rearrangement and must be ortho or para relative to the N-O function.The reaction has been found to be first order in substrate when rates were measured in dioxane, and the activation parameters were calculated.The order of reactivity in this rearrangement is NO2 >> CN > COPh > COMe > COOEt > CONH2.The rates correlate very well with ?- constants and the ρ value was positive and large (+3.6) pointing to a highly po lar activated complex with an electron-rich reaction center.All results strongly support an intramolecular cyclic mechanism.
