- Design, synthesis and biological evaluation of benzamide derivatives as novel NTCP inhibitors that induce apoptosis in HepG2 cells
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Sodium taurocholate cotransport polypeptide (NTCP) plays an important role in the development of hepatitis and acts as a switch to allow hepatitis virus to enter hepatic cells. As the entry receptor protein of hepatitis virus, NTCP is also an effective ta
- Zhao, Shuangmei,Zhen, Yongqi,Fu, Leilei,Gao, Feng,Zhou, Xianli,Huang, Shuai,Zhang, Lan
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supporting information
(2019/08/20)
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- PIPERIDINE DERIVATIVE
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The purpose of the present invention is to provide a compound having excellent antibacterial activity against mycobacterium tuberculosis, multidrug-resistant tuberculosis bacteria, and/or non-tuberculous acid-fast bacteria. A compound represented by formula [I]: (in the formula, each symbol is as described in the attached specification), or a salt thereof can be used to diagnose, prevent, and/or treat tuberculosis.
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Paragraph 0502
(2019/02/19)
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- Synthesis of 2,3-Disubstituted Indoles and Benzofurans by the Tandem Reaction of Rhodium(II)-Catalyzed Intramolecular C-H Insertion and Oxygen-Mediated Oxidation
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A highly effective and straightforward method to construct a wide range of functionalized 2,3-disubstituted indoles has been developed. The method involves the tandem reaction of rhodium(II)-catalyzed denitrogenative annulation of triazole-based benzyl an
- Shen, Hongjuan,Fu, Junkai,Yuan, Hao,Gong, Jianxian,Yang, Zhen
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p. 10180 - 10192
(2016/11/17)
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- Facile and selective deprotection of PMB ethers and esters using oxalyl chloride
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Oxalyl chloride, (0.5 equiv) was found to cleave the PMB group from alkyl, aryl PMB ethers, and esters to give corresponding alcohol and acid in good yields. This method offers simple and efficient protocol for the selective deprotection of PMB ether and ester in DCE at ambient temperature.
- Ilangovan, Andivelu,Anandhan, Karnambaram,Kaushik, Mahabir Prasad
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supporting information
p. 1081 - 1084
(2015/02/19)
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- Organocatalytic route to dihydrocoumarins and dihydroquinolinones in all stereochemical configurations
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A straightforward stereodivergent route to dihydrocoumarins and dihydroquinolinones based on cinchona alkaloid catalyzed addition reactions of monothiomalonates (MTMs) to functionalized nitroolefins followed by deprotection and chemoselective cyclization has been developed. The synthesis proceeds under mild conditions and yields heterocycles with adjacent quaternary and tertiary stereogenic centers in very high yields and stereoselectivities. Moreover, full control over the relative and absolute configuration is achieved by the use of (pseudo)enantiomeric catalysts and the difference in reactivity of thioester versus oxoester moieties. (Chemical Equation Presented).
- Engl, Oliver D.,Fritz, Sven P.,K?slin, Alexander,Wennemers, Helma
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supporting information
p. 5454 - 5457
(2015/02/05)
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- Concise approach to 1,4-dioxygenated xanthones via novel application of the Moore rearrangement
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The rapid synthesis of 1,4-dioxygenated xanthones and related natural products employing the Moore rearrangement as a key transformation has been developed. The approach features an acetylide stitching step to unite a substituted squaric acid with a protected hydroxy benzaldehyde derivative to provide a key intermediate that undergoes facile Moore rearrangement to deliver a hydroxymethyl aryl quinone. Subsequent oxidation, hydroxy group deprotection and cyclization then affords highly functionalized xanthones. The utility of the approach was demonstrated by its application to a concise and efficient synthesis of the naturally-occurring xanthone 1. The structure of a natural product that had been named dulcisxanthone C was also corrected to that of the xanthone 1.
- Nichols, Alexander L.,Zhang, Patricia,Martin, Stephen F.
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experimental part
p. 7591 - 7597
(2012/09/21)
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- Electrophilic carbon transfer in gold catalysis: Synthesis of substituted chromones
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Using easily accessible aromatic alkoxy-arylalkynones, we have investigated the gold-catalyzed intramolecular addition of ethers to alkynes, to give easy access to various substituted chromones. This reaction involves the transfer of the ether substituent via a carbodemetallation process. We also noticed a competing isomerization of several starting materials for which we propose a second gold catalyzed mechanism.
- Renault, Jacques,Qian, Zhao,Uriac, Philippe,Gouault, Nicolas
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supporting information; experimental part
p. 2476 - 2479
(2011/05/16)
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- Convenient access to isoindolinones via carbamoyl radical cyclization. Synthesis of cichorine and 4-hydroxyisoindolin-1-one natural products
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An efficient and convenient access to 2-tert-butylisoindolin-1-ones via an oxidative radical cyclization process from stable carbamoylxanthates, derived from secondary tert-butylamines, is described. The proposed mechanism for this transformation involves, the generation of a carbamoyl radical, its cyclization to the aromatic system, and the dilauroyl peroxide (DLP) mediated rearomatization to generate the isoindolinone ring system. Additionally, the syntheses of cichorine and 4-hydroxyisoindolin-1-one natural products were carried out to underscore the synthetic potential of this xanthate-based carbamoyl radical-oxidative cyclization.
- López-Valdez, Germán,Olguín-Uribe, Simón,Millan-Ortíz, Alejandra,Gamez-Monta?o, Rocio,Miranda, Luis D.
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experimental part
p. 2693 - 2701
(2011/04/24)
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- General and expedient synthesis of 1,4-dioxygenated xanthones
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A facile entry to 1,4-dioxygenated xanthones having a variety of substitution patterns and substituents was developed that features a novel application of the Moore cyclization using substrates that were readily assembled in a highly convergent fashion by an acetylide stitching process. The practical utility of the methodology was demonstrated by an efficient synthesis of a naturally occurring xanthone and correction of the structure of dulcisxanthone C.
- Nichols, Alexander L.,Zhang, Patricia,Martin, Stephen F.
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supporting information; experimental part
p. 4696 - 4699
(2011/10/09)
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- Efficient preparation and processing of the 4-methoxybenzyl (PMB) group for phenolic protection using ultrasound
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(Chemical Equation Presented) Power ultrasound efficiently facilitates the rapid preparation and reaction of 4-methoxybenzyl chloride (PMB-Cl) 1 in providing protected phenolic ether intermediates for organic synthesis. Using two-phase systems in both the ultrasound-promoted preparation and reactions of PMB-Cl, typical runs produce PMB-protected products within 15 min. When compared with nonsonicated control reactions, the results demonstrate clear advantage in terms of efficiency when the protocol is applied to the mild and selective protection of various multisubstituted phenols including sensitive phenolic aldehydes.
- Luzzio, Frederick A.,Chen, Juan
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p. 5621 - 5624
(2008/12/21)
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- PYRROLE COMPOUNDS FOR THE TREATMENT OF PROSTAGLANDIN MEDIATED DISEASES
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Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein A, R1, R2a, R2b, Rx, R8, and R9 are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine, in particular their use in the treatment of prostaglandin mediated diseases such as pain, inflammatory, immunological, bone, neurodegenerative or renal disorder.
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