Synthesis method and applications of N heteroatom polysubstituted benzoquaternary cycloketone
The invention discloses an N heteroatom polysubstituted benzoquaternary cycloketone synthesis method. According to the invention, the synthetic route starts from a known aniline compound A, the hundred g-scale preparation can be achieved, the yield can ac
-
Paragraph 0075; 0081-0084
(2020/03/12)
Cyclopentadienyl molybdenum(II) compounds bearing carboxylic acid functional group
This work describes a procedure giving cyclopentadienyl molybdenum(II) compounds bearing carboxylic acid function group. It involves synthesis of carboxylic acid ester functionalized cyclopentadienides, their coordination to molybdenum(II) precursor and saponification of ester function groups. The method is not limited only to compounds with the function group directly attached in the cyclopentadienyl ring but also to those functionalized in the side chain. The attempts to synthesize the indenyl analogues were only partially successful due to low stability in the saponification step. All reported structure types were elucidated from spectroscopic measurements and verified by X-ray crystallography. The second part of the work describes an effect of the outer-coordination sphere on cytotoxicity of the cationic molybdenum(II) compounds bearing N,N-chelating ligands. The cytotoxicity of the modified species bearing phenanthroline ligand toward human leukemia cells MOLT-4 (IC50 = 10.5 ± 0.5 μmol l?1) is higher than reported for cisplatin (IC50 = 15.8 ± 1.9 μmol l?1).
Schejbal, Ji?í,Melounková, Lucie,Vinklárek, Jaromír,?ezá?ová, Martina,R??i?ková, Zdeňka,Císa?ová, Ivana,Honzí?ek, Jan
p. 66 - 73
(2018/05/09)
Catalytic Enantioselective Synthesis of 3,4-Polyfused Oxindoles with Quaternary All-Carbon Stereocenters: A Rh-Catalyzed C-C Activation Approach
The first Rh-catalyzed enantioselective synthesis of a 3,4-polyfused oxindole ring system enabled by carboacylation of acrylic amides based on C-C activation is reported. This transformation provides a new entry to access 3,4-polyfused oxindoles bearing q
Qiu, Bo,Li, Xiao-Tong,Zhang, Jian-Yu,Zhan, Jun-Ling,Huang, Shuang-Ping,Xu, Tao
supporting information
p. 7689 - 7693
(2018/12/14)
Kinetic analysis of the inhibition of phenylalanine ammonia-lyase by 2-aminoindan-2-phosphonic acid and other phenylalanine analogues
The conformationally restricted phenylalanine analogue 2-aminoindan-2-phosphonic acid (AIP) inhibits phenylalanine ammonialyase (PAL) competitively in a time-dependent manner. This phenomenon was investigated in more detail with the heterologously expressed, highly purified homotetrameric PAL-1 isozyme from parsley. The kinetic analysis revealed that the enzyme-inhibitor complex is formed in a single "slow" step with an association rate of k2 = 2.6±0.04 104 M-1 s-1. The inhibition is reversible with a dissociation rate of k-2 = 1.8±0.04 10-4 s-1 and an equilibrium constant of Ki = 7±2 nM. The previously described PAL inhibitor (S)-2-aminooxy-3-phenylpropanoic acid [(S)-AOPP] was also found to be a slow-binding inhibitor of PAL-1. The carboxyl analogue of AIP, 2-aminoindan-2-carboxylic acid, served as a substrate of PAL-1 and was converted to indene-2-carboxylic acid.
Appert, Christoph,Zon, Jerzy,Amrhein, Nikolaus
p. 415 - 422
(2007/10/03)
More Articles about upstream products of 43073-37-6