104014-46-2Relevant articles and documents
Chemoselective Alkylation of Aminoacetophenones with Alcohols by Using a Palladacycle-Phosphine Catalyst
Mamidala, Ramesh,Subramani, M. Siva,Samser, Shaikh,Biswal, Priyabrata,Venkatasubbaiah, Krishnan
, p. 6286 - 6296 (2018)
The development of efficient and environmentally benign palladacycle-phosphine catalyzed process to enable the formation of chemoselective C-alkylated or N-alkylated aminoacetophenones with alcohols is described. This methodology proved to be tunable by variation of the base and the temperature, which allows for the isolation of structurally diverse C-alkylated and N-alkylated aminoacetophenones. Moreover, this methodology has been applied to the synthesis of biologically and industrially important donepezil.
Efficient photocatalytic one-pot hydrogenation and N-alkylation of nitrobenzenes/benzonitriles with alcohols over Pd/MOFs: Effect of the crystal morphology & “quasi-MOF” structure
Bian, Fengxia,Cheng, Hongmei,Jiang, Heyan,Liu, Xingyan,Long, Xingyu,Yang, Chaofen
, p. 121 - 131 (2020/06/23)
One-pot multi-step reactions over visible-light induced catalysis feature the sustainable green process. Here, ligand structure change and 2-MI coordinated modulation were adapted to adjust the crystal size, morphology and crystalline structure of Fe-MOFs; double solvent impregnation was employed for the Pd loading; “quasi-MOF” materials with retained morphology were formed with calcination under N2. Above modified materials were employed as multifunctional photocatalysts for highly efficient one-pot hydrogenation and N-alkylation of nitrobenzenes or benzonitriles with alcohols after in situ Pd photoreduction. Photocatalytic performance was evidently affected by the Fe-MOFs crystal size, morphology, crystalline structure alteration and “quasi-MOF” construction. One-pot hydrogenation and N-alkylation of benzonitriles with alcohols was achieved with excellent catalytic performance firstly in heteroegeneous catalysis. Reaction mechanism was proposed with the assistance of in situ DRIFTS.
Organometallic titanocene complex as highly efficient bifunctional catalyst for intramolecular Mannich reaction
Wang, Yunyun,Jian, Yajun,Wu, Ya,Sun, Huaming,Zhang, Guofang,Zhang, Weiqiang,Gao, Ziwei
, (2019/05/07)
Bifunctional catalysts bearing two catalytic sites, Lewis acidic organometallic titanocene and Br?nsted acidic COOH, have been assembled in situ from Cp2TiCl2 with carboxylic acid ligands, showing high catalytic activity over an intramolecular Mannich reaction towards synthesis of 2-aryl-2,3-dihydroquinolin-4(1H)-ones. The determination of the bifunctional catalyst Cp2Ti(C8H4NO6)2 was elucidated by single X-ray HR-MS and investigation of catalytic behavior. In particular, masking the Br?nsted acidic COOH catalytic site with dormant COOMe lowered the reaction yield greatly, indicating that two catalytic sites work together to maintain high catalytic efficiency.
Design, synthesis and biological activity of selective hCAs inhibitors based on 2-(benzylsulfinyl)benzoic acid scaffold
Rotondi, Giulia,Guglielmi, Paolo,Carradori, Simone,Secci, Daniela,De Monte, Celeste,De Filippis, Barbara,Maccallini, Cristina,Amoroso, Rosa,Cirilli, Roberto,Akdemir, Atilla,Angeli, Andrea,Supuran, Claudiu T.
, p. 1400 - 1413 (2019/08/26)
A large library of derivatives based on the scaffold of 2-(benzylsulfinyl)benzoic acid were synthesised and tested as atypical inhibitors against four different isoforms of human carbonic anhydrase (hCA I, II, IX and XII, EC 4.2.1.1). The exploration of the chemical space around the main functional groups led to the discovery of selective hCA IX inhibitors in the micromolar/nanomolar range, thus establishing robust structure-activity relationships within this versatile scaffold. HPLC separation of some selected chiral compounds and biological evaluation of the corresponding enantiomers was performed along with molecular modelling studies on the most active derivatives.
