619-21-6Relevant articles and documents
A Magnetically Recyclable Palladium-Catalyzed Formylation of Aryl Iodides with Formic Acid as CO Source: A Practical Access to Aromatic Aldehydes
You, Shengyong,Zhang, Rongli,Cai, Mingzhong
, p. 1962 - 1970 (2021/01/25)
A magnetically recyclable palladium-catalyzed formylation of aryl iodides under CO gas-free conditions has been developed by using a bidentate phosphine ligand-modified magnetic nanoparticles-anchored- palladium(II) complex [2P-Fe 3O 4@SiO 2-Pd(OAc) 2] as catalyst, yielding a wide variety of aromatic aldehydes in moderate to excellent yields. Here, formic acid was employed as both the CO source and the hydrogen donor with iodine and PPh 3as the activators. This immobilized palladium catalyst can be obtained via a simple preparative procedure and can be facilely recovered simply by using an external magnetic field, and reused at least 9 times without any apparent loss of catalytic activity.
Preparation method of 3-carboxybenzaldehyde
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Paragraph 0040; 0043; 0045; 0048; 0050; 0053, (2020/04/29)
The invention discloses a preparation method of 3-carboxybenzaldehyde. The method comprises the following steps: by using m-toluonitrile as a starting raw material, carrying out a first hydrolysis reaction, and adding an acid to carry out an acidification reaction to obtain m-toluic acid; carrying out chlorination reaction on m-toluic acid to obtain 3-carboxyl benzyl chloride; mixing the 3-carboxyl benzyl chloride and urotropin for an oxidation reaction, then adding glacial acetic acid and water for a second hydrolysis reaction to obtain the 3-carboxybenzaldehyde. According to the method disclosed by the invention, m-toluonitrile with low cost is used as a raw material, the 3-carboxybenzaldehyde is synthesized through a series of processes of hydrolysis, chlorination, oxidation and hydrolysis, and the product purity and yield are relatively high; the method has the advantages of simple and safe process operation, easily available raw materials and low cost and is suitable for industrial production.
Bisubstrate inhibitors of nicotinamide N-methyltransferase (NNMT) with enhanced activity
Gao, Yongzhi,Van Haren, Matthijs J.,Moret, Ed E.,Rood, Johannes J. M.,Sartini, Davide,Salvucci, Alessia,Emanuelli, Monica,Craveur, Pierrick,Babault, Nicolas,Jin, Jian,Martin, Nathaniel I.
, p. 6597 - 6614 (2019/08/20)
Nicotinamide N-methyltransferase (NNMT) catalyzes the methylation of nicotinamide to form N-methylnicotinamide. Overexpression of NNMT is associated with a variety of diseases, including a number of cancers and metabolic disorders, suggesting a role for NNMT as a potential therapeutic target. By structural modification of a lead NNMT inhibitor previously developed in our group, we prepared a diverse library of inhibitors to probe the different regions of the enzyme's active site. This investigation revealed that incorporation of a naphthalene moiety, intended to bind the hydrophobic nicotinamide binding pocket via π-πstacking interactions, significantly increases the activity of bisubstrate-like NNMT inhibitors (half-maximal inhibitory concentration 1.41 μM). These findings are further supported by isothermal titration calorimetry binding assays as well as modeling studies. The most active NNMT inhibitor identified in the present study demonstrated a dose-dependent inhibitory effect on the cell proliferation of the HSC-2 human oral cancer cell line.
