125652-30-4Relevant academic research and scientific papers
The synthesis of rigid polycyclic structures for the study of diatropic or steric effects of a phenyl ring on CF bond
Chang, Yung-Yu,Ho, I-Ting,Ho, Tse-Lok,Chung, Wen-Sheng
, p. 12790 - 12794 (2013)
Polycyclic compounds 1a-c were synthesized to study the diatropic effects of a flanking phenyl ring on nearby CH and CF bonds. 19F NMR spectra of 1b and 1c were strongly deshielded compared with those of the ring-opened compounds 3b, 7b, and 7c
Synthesis and biological evaluation of novel 1,2,4-triazine derivatives bearing carbazole moiety as potent α-glucosidase inhibitors
Wang, Guangcheng,Wang, Jing,He, Dianxiong,Li, Xin,Li, Juan,Peng, Zhiyun
, p. 2806 - 2809 (2016)
A new series of 1,2,4-triazine derivatives bearing carbazole moiety 7a-7p were designed, synthesized, and evaluated for their α-glucosidase inhibitory activity. The majority of the screened compounds displayed potent α-glucosidase inhibitory activity, with IC50 values in the range of 4.27 ± 0.07-47.75 ± 0.25 μM as compared to the standard drug acarbose. Among the series, compound 7k represented the most potent α-glucosidase inhibitory activity with IC50 values of 4.27 ± 0.07 μM. Kinetic analysis revealed that compound 7k is a non-competitive inhibitor with a Ki of 4.43 μM. Furthermore, the binding interactions of compound 7k with α-glucosidase was confirmed through molecular docking. This study showed these 1,2,4-triazine derivatives bearing carbazole moiety as a new class of α-glucosidase inhibitors.
Zinc salt-catalyzed reduction of α-aryl imino esters, diketones and phenylacetylenes with water as hydrogen source
Shen, Guoli,Liu, Haojie,Chen, Jingchao,He, Zhenxiu,Zhou, Yongyun,Wang, Lin,Luo, Yang,Su, Zhimin,Fan, Baomin
supporting information, p. 3601 - 3610 (2021/05/04)
The zinc salt-catalyzed reduction of α-aryl imino esters, diketones and phenylacetylenes with water as hydrogen source and zinc as reductant was successfully conducted. The presented method provides a low-cost, environmentally friendly and practical preparation of α-aryl amino esters, α-hydroxyketones and phenylethylenes. By using D2O as deuterium source, the corresponding products were obtained in high efficiency with excellent deuterium incorporation rate, which gives a cheap and safe tool for access to valuable deuterium-labelled compounds. This journal is
Base-Free Asymmetric Transfer Hydrogenation of 1,2-Di- and Monoketones Catalyzed by a (NH)2P2-Macrocyclic Iron(II) Hydride
De Luca, Lorena,Mezzetti, Antonio
supporting information, p. 11949 - 11953 (2017/09/20)
The hydride isonitrile complex [FeH(CNCEt3)(1 a)]BF4 (2) containing a chiral P2(NH)2 macrocycle (1 a), in the presence of 2-propanol as hydrogen donor, catalyzes the base-free asymmetric transfer hydrogenation (ATH) of prostereogenic ketones to alcohols and the hemihydrogenation of benzils to benzoins, which contain a base-labile stereocenter. Benzoins are formed in up to 83 % isolated yield with enantioselectivity reaching 95 % ee. Ketones give the same enantioselectivity observed with the parent catalytic system [Fe(CNCEt3)2(1 a)] (3 a) that operates with added NaOtBu.
COMPOUNDS AND USES THEREOF IN THE TREATMENT OF CANCERS AND OTHER MEDICAL CONDITIONS
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Paragraph 0101; 0103; 0109; 00128, (2017/02/09)
There are provided compounds, their preparation and their use in the treatment of medical conditions including cancers and immune disorders.
Chemoselective and repetitive intermolecular cross-acyloin condensation reactions between a variety of aromatic and aliphatic aldehydes using a robust N-heterocyclic carbene catalyst
Jin, Ming Yu,Kim, Sun Min,Mao, Hui,Ryu, Do Hyun,Song, Choong Eui,Yang, Jung Woon
supporting information, p. 1547 - 1550 (2014/03/21)
We found that chemoselectivity of the crossed acyloin product is controlled by the adjustment of the aromatic aldehyde/aliphatic aldehyde ratio. Moreover, we observed the persistent catalytic activity of the homogeneous NHC catalyst in a solution due to N
N-heterocyclic carbene-catalyzed annulation of α-cyano-1,4-diketones with ynals
Romanov-Michailidis, Fedor,Besnard, Celine,Alexakis, Alexandre
supporting information, p. 4906 - 4909,4 (2012/12/12)
In this paper, the first stereoselective annulation reaction between r-cyano-1,4-diketones and ynals, mediated by catalytic amounts of a triazolium salt precatalyst and cocatalytic amounts of a weak carboxylate base, is disclosed. The title transformation proceeds smoothly under mild reaction conditions and generates three contiguous stereogenic centers, one of which is a quaternary acetal carbon. This reaction tolerates a wide variety of electronically distinct substituents on both reaction partners and affords privileged bicyclic scaffolds in 61-90% isolated yields and with up to 20:1 diastereomeric preference.
N-heterocyclic carbene-catalyzed annulation of α-cyano-1,4-diketones with ynals
Romanov-Michailidis, Fedor,Besnard, Céline,Alexakis, Alexandre
supporting information, p. 4906 - 4909 (2013/01/15)
In this paper, the first stereoselective annulation reaction between r-cyano-1,4-diketones and ynals, mediated by catalytic amounts of a triazolium salt precatalyst and cocatalytic amounts of a weak carboxylate base, is disclosed. The title transformation proceeds smoothly under mild reaction conditions and generates three contiguous stereogenic centers, one of which is a quaternary acetal carbon. This reaction tolerates a wide variety of electronically distinct substituents on both reaction partners and affords privileged bicyclic scaffolds in 61-90% isolated yields and with up to 20:1 diastereomeric preference.
One-pot synthesis of quinoxalines starting from aldehydes under metal-free conditions
Hu, Zhong-Yuan,Du, Ding,Tang, Wei-Fang,Lu, Tao
experimental part, p. 2262 - 2264 (2012/08/07)
An efficient and convenient synthesis of quinoxalines from easily available aldehydes was performed as a one-pot procedure in good to excellent yields under metal-free conditions, via sequential benzoin condensation, aerobic formation of benzils and condensation of the latter with 1,2-diaminobenzenes.
