A biocatalytic approach for the production of (S)-N-(2-ethyl-6-methylphenyl)alanine, a key intermediate for (S)-Metolachlor, has been developed by the use of lipase-catalyzed hydrolytic kinetic resolution. Compared with other selected lipases, the lipase from Pseudomonas cepacia (PSL) gives good...
The enzyme (BSL2), a highly active lipase expressed from newly constructed strain of Bacillus subtilis BSL2, is used in the kinetic resolution of N-(2-ethyl-6-methylphenyl)alanine from the corresponding racemic methyl ester. Reaction conditions are optimized to enhance the enantioselectivity. Th...
Pseudomonas sp. Lipase (PSL) immobilized with the method of cross-linked enzyme aggregates (CLEAs) using acetone as the optimal precipitant is investigated. The immobilization efficiency (%) and activity retention (%) of the immobilized lipase (CLEA-PSL) are 70.6 and 45.1%, respectively. In the ...
Dengue virus is endemic throughout tropical and subtropical regions, and cause severe epidemic diseases. The NS2B/NS3 protease is a promising drug target for dengue virus. Herein, we report the discovery and modification of a novel class of thiadiazoloacrylamide derivatives with potent inhibitor...
A mild and efficient copper-catalyzed oxidative trifluoroethoxylation of aryl and heteroaryl boronic acids with CF3CH2OH has been developed. This protocol tolerates a range of functional groups, allowing access to a variety of aryl and heteroaryl trifluoroethyl ethers.
A copper-mediated oxidative pentafluoroethylthiolation of aryl boronic acids with TMSC2F5 and S8 was developed. This reaction provides a new access to various aryl pentafluoroethyl thioethers. The use of 2-fluoropyridine as the ligand and the ability to carry out the reaction at 70 °C are key f...
The rapid rise of antimicrobial resistance is one of the greatest challenges currently facing medical science. The most common cause of resistance to β-lactam antibiotics is the expression of β-lactamase enzymes, such as KPC-2. As such the development of novel inhibitors of KPC-2 and related e...
Owing to the unusual reactivity of dialkylamine-borane complexes, a methodology was developed to simply access boronic acids. The intrinsic instability of magnesium aminoborohydride was tweaked into a tandem dehydrogenation borylation sequence. Proceeding via an autocatalytic cycle, amineborane ...
Sewage sludge of biological wastewater treatment plant was converted into sewage sludge based activated carbon (SBAC) with ZnCl2 as activation agent, which supported manganese and ferric oxides as catalysts (including SBAC) to improve the performance of ozonation of real biologically pretreated ...
Tiazofurin analogues bearing a 5-hydroxymethyl-2-methyl-tetrahydrofuro[2,3-d][1,3]dioxol-6-ol moiety as a sugar mimic (2 and 3), and two novel thiazole-based acyclo-C-nucleosides 4 and 16 have been synthesized in multistep sequences starting from d-xylose (compounds 2 and 3) or from d-arabinose ...
Cyclic trimers of 3-(N-alkylamino)benzoic acid (calix[3]amides) with various substituents at the meta position of the phenyl rings were synthesized and the effects of the substituents on the crystal structures and energy profiles in solution were examined. The calixamides existed in a syn confor...
An efficient synthesis of methyl ketones from terminal olefins using PdCl2/CrO3 system mimicking the Wacker process is developed. The method shows good functional groups compatibility, no aldehyde by-products and is operationally simple. CrO3 is the sole oxidant and replaces both Cu-salts and mo...
The rate constants for acetolysis of (2,2-difluorocyclopropyl)methyl tosylate, and (2,2-difluoro-3-methylcyclopropyl)methyl tosylate at 92 °C and of 1-(2,2-difluorocyclopropyl)ethyl tosylate at 42 °C are reported and the reactivities and regiochemistries of ring opening of these systems are di...
Current study is based on the biology-oriented drug synthesis (BIODS) of 2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl aryl carboxylate derivatives 1–26, by treating metronidazole with different aryl and hetero-aryl carboxylic acids in the presence of 1,1′-carbonyl diimidazole (CDI) as a coupling...
In recent years, the imine-bridged organics has been one of the hot spots in the field of photo-responsive materials. Herein, N-(5-chloro-2-hydroxyphenyl)-(3-bromo-6-oxocyclohexa-2,4-dienylidene)-methylamine (CHPBOCDMA) was synthesized and characterized by a combined experimental and theoretical...
We have made an effort to synthesize ternary complexes [Cu2(L)2(Him)2]·CH3OH 1, [Cu(L)(bipy)] 2 and [Ni(HL)(PMDT)]BF4 3 (H2L = N′-(1E)-[(5-bromo-2-hydroxyphenyl)methylidene]benzoylhydrazone; Him = imidazole; bipy = 2,2′-bipyridine and PMDT = N,N,N′,N″,N″-pentamethyldiethylenetriamine). The...
Plastics are indispensable for our comfortable life. But, they are easily degraded by autoxidation, especially under the action of UV light, due to their organic character. Therefore, additives preventing the photo-oxidation are needed. 2-Hydroxybenzophenones are widely used as ultraviolet absor...
The reagent 2-nitro-5-thiocyanatobenzoic acid (NTCB) is commonly used to cyanylate and cleave proteins at cysteine residues, but this two-step reaction requires lengthy incubations and produces highly incomplete cleavages. In previous reports, incomplete cleavage was attributed to a competing β...
In this work, performance analysis and characterization of flat sheet polyamide RO membrane for simultaneous rejection of fluoride and Cr(VI) from Synthetic binary water system were carried. Simultaneous rejection of fluoride and Cr(VI) ions was conducted at different operational conditions. Max...
Hexavalent chromium (Cr(VI)) is a well-known human carcinogen and a strong oxidizer that causes severe DNA damage. However, the associations between epigenetic dysregulation and DNA damage have not been well-characterized. In this study, we evaluated the effects of short-term and long-term expos...
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