57999-46-9Relevant academic research and scientific papers
Design, synthesis and biological evaluation of 2-substituted-6-[(4-substituted-1-piperidyl)methyl]-1H-benzimidazoles as inhibitors of ebola virus infection
Bessières, Maxime,Plebanek, El?bieta,Chatterjee, Payel,Shrivastava-Ranjan, Punya,Flint, Mike,Spiropoulou, Christina F.,Warszycki, Dawid,Bojarski, Andrzej J.,Roy, Vincent,Agrofoglio, Luigi A.
, (2021/02/06)
Novel 2-substituted-6-[(4-substituted-1-piperidyl)methyl]-1H-benzimidazoles were designed and synthesized as Ebola virus inhibitors. The proposed structures of the new prepared benzimidazole-piperidine hybrids were confirmed based on their spectral data and CHN analyses. The target compounds were screened in vitro for their anti-Ebola activity. Among tested molecules, compounds 26a (EC50=0.93 μM, SI = 10) and 25a (EC50=0.64 μM, SI = 20) were as potent as and more selective than Toremifene reference drug (EC50 = 0.38 μM, SI = 7) against cell line. Data suggests that the mechanism by which 25a and 26a block EBOV infection is through the inhibition of viral entry at the level of NPC1. Furthermore, a docking study revealed that several of the NPC1 amino acids that participate in binding to GP are involved in the binding of the most active compounds 25a and 26a. Finally, in silico ADME prediction indicates that 26a is an idealy drug-like candidate. Our results could enable the development of small molecule drug capable of inhibiting Ebola virus, especially at the viral entry step.
Bimetal complex with aryloxy ether skeleton, and preparation method and application thereof
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Paragraph 0129; 0143-0144, (2020/11/26)
The invention provides a bimetallic complex with an aryloxy ether skeleton, and a preparation method and application of the bimetallic complex. The bimetallic complex has a structural expression as shown in the specification. A catalytic system of the bimetallic complex shows very good catalytic activity and thermal stability when being used for catalyzing olefin homopolymerization or olefin/alphaolefin copolymerization reactions, and a polymerization product generated by catalysis has relatively high molecular weight and a high alpha-olefin insertion rate and has a very good industrial application prospect.
IVB group-containing bimetallic complex catalyst as well as preparation method and application thereof
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Paragraph 0111; 0113; 0122-0125, (2020/11/23)
The invention provides an IVB group-containing bimetallic complex catalyst as well as a preparation method and application of the catalyst. The IVB group-containing bimetallic complex has a structuralexpression shown in the specification. The IVB group-co
Asymmetric Transfer Hydrogenation of o-Hydroxyphenyl Ketones: Utilizing Directing Effects That Optimize the Asymmetric Synthesis of Challenging Alcohols
Clarkson, Guy J.,Wills, Martin,Zheng, Ye
supporting information, (2020/05/05)
A systematic range of o-hydroxyphenyl ketones were reduced under asymmetric transfer hydrogenation conditions using the C3-tethered catalyst 2. Two directing effects, i.e., an o-hydroxyphenyl coupled to a bulky aromatic on the opposite side of the ketone substrate, combine in a matched manner to deliver reduction products with very high enantiomeric excess.
Metal complex, preparation method and application thereof
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Paragraph 0125; 0136-0140, (2020/10/20)
The invention provides a metal complex, a preparation method and application thereof. The metal complex has the following structural expression shown as the specification. The invention has the technical advantages that: the invention puts forward the O,
Enantioselective (3+2) cycloaddition: Via N-heterocyclic carbene-catalyzed addition of homoenolates to cyclic N -sulfonyl trifluoromethylated ketimines: Synthesis of fused N-heterocycle γ-lactams
Zhang, Zhen-Zhen,Zhang, Yongna,Duan, Hui-Xin,Deng, Zhuo-Fei,Wang, You-Qing
supporting information, p. 1553 - 1556 (2020/02/13)
An enantioselective (3+2) cycloaddition of enals and cyclic N-sulfonyl trifluoromethyl ketimines via N-heterocyclic carbene-catalyzed homoenolate addition is described. This reaction can efficiently construct fused N-heterocycle γ-lactams bearing two adjacent chiral centers with >20?:?1 dr and 94-99% ee, with one chiral center as a trifluoromethylated α-tetrasubstituted carbon stereocenter.
Cascade Claisen and Meinwald Rearrangement for One-Pot Divergent Synthesis of Benzofurans and 2 H-Chromenes
Song, Liyan,Su, Qian,Lin, Xi,Du, Zhihui,Xu, Huiyou,Ouyang, Ming-An,Yao, Hongliang,Tong, Rongbiao
supporting information, p. 3004 - 3009 (2020/04/20)
A new cascade approach has been developed for the one-pot four-step divergent synthesis of polysubstituted benzofurans and 2H-chromenes, featuring a novel cascade aromatic Claisen rearrangement/Meinwald rearrangement/dehydrative or oxidative cyclization. This new method was demonstrated with 39 examples tolerating different substitutions at an epoxide, allylic ether, and aromatic ring, and we showcased its utility with the first total synthesis of natural product liparacid A in seven steps.
Formation and Activation of Zr/Hf Bis(phenolate-ether) Precatalysts
Cuthbert, Eric N. T.,Busico, Vincenzo,Herbert, David E.,Budzelaar, Peter H. M.
supporting information, p. 3396 - 3410 (2019/08/12)
Zr and Hf complexes of bis(phenolate-ether) (“O4”) ligands feature high activity, stereoselectivity and molecular weight capability for propene polymerization at high temperature. Here we report a simplified ligand synthesis and several new examples of O4
Ru(II)-catalyzed C-H activation and annulation of salicylaldehydes with monosubstituted and disubstituted alkynes
Baruah, Swagata,Kaishap, Partha Pratim,Gogoi, Sanjib
supporting information, p. 13004 - 13007 (2016/11/11)
The Ru(ii)-catalyzed C-H activation and annulation reaction of salicylaldehydes and disubstituted alkynes affords chromones in high yields. This reaction also works with terminal alkynes and tolerates a wide range of sensitive functional groups. The selectivity pattern of this Ru(ii)-catalyzed annulation reaction is different from the known Au(i), Rh(iii)-catalyzed annulation reactions of salicylaldehydes and terminal alkynes.
Synthesis of Phenanthrene Derivatives by Intramolecular Cyclization Utilizing the [1,2]-Phospha-Brook Rearrangement Catalyzed by a Bronsted Base
Kondoh, Azusa,Aoki, Takuma,Terada, Masahiro
supporting information, p. 12577 - 12580 (2015/09/01)
The synthesis of functionalized phenanthrene derivatives was achieved by intramolecular cyclization utilizing the [1,2]-phospha-Brook rearrangement under Bronsted base catalysis. Treatment of biaryl compounds having an α-ketoester moiety and an alkyne moiety at the 2 and 2′ positions, respectively, with diisopropyl phosphite in the presence of a catalytic amount of phosphazene base P2-tBu provides 9,10-disubstituted phenanthrene derivatives in high yields. This reaction involves the generation of an ester enolate through an umpolung process, that is, addition of diisopropyl phosphite to a keto moiety followed by the [1,2]-phospha-Brook rearrangement, the intramolecular addition to an alkyne, and the [3,3] rearrangement of the allylic phosphate moiety in a consecutive fashion.
