87770-86-3Relevant academic research and scientific papers
ARGININE GINGIPAIN INHIBITORS
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Paragraph 0134, (2020/10/09)
Therapeutics targeting the bacterium Porphyromonas gingivalis, including its proteases arginine gingipain A and arginine gingipain B, are disclosed, as well as the use thereof for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease. In certain embodiments, the invention provides compounds according to Formula I, Formula Ia, and Formula Ib, as described herein, and pharmaceutically acceptable salts thereof.
Esterase-Triggered Self-Immolative Thiocarbamates Provide Insights into COS Cytotoxicity
Levinn, Carolyn M.,Steiger, Andrea K.,Pluth, Michael D.
, (2019/01/25)
Hydrogen sulfide (H2S) is an important gasotransmitter and biomolecule, and many synthetic small-molecule H2S donors have been developed for H2S-related research. One important class of triggerable H2S donors is
Selective Hydroboration of Carboxylic Acids with a Homogeneous Manganese Catalyst
Barman, Milan K.,Das, Kuhali,Maji, Biplab
, p. 1570 - 1579 (2019/01/30)
Catalytic reduction of carboxylic acid to the corresponding alcohol is a challenging task of great importance for the production of a variety of value-added chemicals. Herein, a manganese-catalyzed chemoselective hydroboration of carboxylic acids has been developed with a high turnover number (>99?000) and turnover frequency (>2000 h-1) at 25 °C. This method displayed tolerance of electronically and sterically differentiated substrates with high chemoselectivity. Importantly, aliphatic long-chain fatty acids, including biomass-derived compounds, can efficiently be reduced. Mechanistic studies revealed that the reaction occurs through the formation of active manganese-hydride species via an insertion and bond metathesis type mechanism.
Preparation method for synthesis of phenolic ester through thiocarboxylic acid mediated visible light catalyzed phenol acylation reaction
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Paragraph 0017; 0018; 0059; 0060; 0061, (2018/07/30)
The invention discloses a preparation method for synthesis of phenolic ester through a thiocarboxylic acid mediated visible light catalyzed phenol acylation reaction. Thiocarboxylic acid compounds andphenol compounds are subjected to a site specific reaction under certain conditions to produce phenolic ester compounds, wherein the certain conditions are as follows: under the conditions of normaltemperature, normal pressure and visible light, K2CO3 is used as an alkaline catalyst, terpyridyl ruthenium dichloride hexahydrate is used as a photosensitizer and acetonitrile is used as a reaction solvent. Synthesis of phenolic ester under catalysis of visible light is realized, thiocarboxylic acid is used as an acylation reagent, and the site specific phenol esterification reaction is realizedefficiently under mild conditions of normal temperature, normal pressure and visible light. The method has mild reaction conditions, large substrate functional group tolerance, high applicability andhigh yield, and an efficient, reliable and economical preparation method is provided for synthesis of phenolic ester.
Diacyl Disulfide: A Reagent for Chemoselective Acylation of Phenols Enabled by 4-(N,N-Dimethylamino)pyridine Catalysis
Liu, Hong-Xin,Dang, Ya-Qian,Yuan, Yun-Fei,Xu, Zhi-Fang,Qiu, Sheng-Xiang,Tan, Hai-Bo
supporting information, p. 5584 - 5587 (2016/11/17)
A general and excellent acylation reagent, diacyl disulfide, was uncovered for efficient ester formation enabled by DMAP (4-(N,N-dimethylamino)pyridine) catalysis. This protocol offered a promising synthetic platform on site-selective acylation of phenolic and primary aliphatic hydroxyl groups, which greatly expanded the realm of protecting group chemistry. The importance of the reagent was also reflected by its excellent moisture tolerance, high efficiency, and potential in synthetic chemistry and biologically meaningful natural product modification.
Palladium Catalysis Enables Benzylation of α,α-Difluoroketone Enolates
Yang, Ming-Hsiu,Hunt, Jordan R.,Sharifi, Niusha,Altman, Ryan A.
supporting information, p. 9080 - 9083 (2016/07/26)
A palladium-catalyzed decarboxylative benzylation reaction of α,α-difluoroketone enolates is reported, in which the key C(α)?C(sp3) bond is generated by reductive elimination from a palladium intermediate. The transformation provides convergent access to α-benzyl-α,α-difluoroketone-based products, and should be useful for accessing biological probes.
Bis(benzoyloxybenzyl)-DiPPro nucleoside diphosphates of anti-HIV active nucleoside analogues
Weinschenk, Lina,Gollnest, Tristan,Schols, Dominique,Balzarini, Jan,Meier, Chris
, p. 891 - 900 (2015/05/05)
Nucleoside analogues are extensively used as antiviral and anticancer agents. Their efficiency is dependent on their metabolism into the ultimately active nucleoside triphosphates. Often one step or even more in the metabolism of the nucleoside to the tri
COMPOUNDS USEFUL IN THE TREATMENT OF NEOPLASTIC DISEASES
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, (2015/04/15)
The present invention refers to compounds of formula: (formula A), wherein R1 is selected from (formula I), (formula II), (formula (III), (formula IV), (formula V), or (formula B), and wherein R2, R3, R4 and Rs
Iridium-catalyzed dehydrogenative decarbonylation of primary alcohols with the liberation of syngas
Olsen, Esben P. K.,Madsen, Robert
supporting information, p. 16023 - 16029 (2013/02/22)
A new iridium-catalyzed reaction in which molecular hydrogen and carbon monoxide are cleaved from primary alcohols in the absence of any stoichiometric additives has been developed. The dehydrogenative decarbonylation was achieved with a catalyst generated in situ from [Ir(coe)2Cl]2 (coe=cyclooctene) and racemic 2,2'-bis(diphenylphosphino)-1,1'-binaphthyl (rac-BINAP) in a mesitylene solution saturated with water. A catalytic amount of lithium chloride was also added to improve the catalyst turnover. The reaction has been applied to a variety of primary alcohols and gives rise to products in good to excellent yields. Ethers, esters, imides, and aryl halides are stable under the reaction conditions, whereas olefins are partially saturated. The reaction is believed to proceed by two consecutive organometallic transformations that are catalyzed by the same iridium(I)-BINAP species. First, dehydrogenation of the primary alcohol to the corresponding aldehyde takes place, which is then followed by decarbonylation to the product with one less carbon atom.
