The SmCo alloy waste is considered to be one of the most valuable wastes for recycling, primarily due to the value of the Co and Sm metals. The two metals were extracted from the SmCo alloy waste by sulfuric acid leaching, and Sm(III) was separated by sodium sulfate as a precipitate of sodium sa...
The cyclic AMP (cAMP) signaling pathway is implicated in the development of alcohol use disorder. Previous studies have demonstrated that ethanol enhances the activity of adenylyl cyclase (AC) in an isoform specific manner; AC7 is most enhanced by ethanol, and regions responsible for enhancement...
Treatment of 1-chlorovinyl p-tolyl sulfoxides, which were synthesized from cyclic ketones and chloromethyl p-tolyl sulfoxide in three steps in good yields, with N-lithio arylamines gave sulfinylaziridines in high yields. On treatment with N-lithio aniline or N-lithio p-chloroaniline, the sulfiny...
Addition of the carbanion of chloromethyl phenyl sulfoxide to ketones gave the adducts, which were treated with lithium diisopropylamide to afford one-carbon homologated α-sulfinyl ketones via α-sulfinyl carbenoids in moderate to high yields.
Treatment of lithium α-sulfinyl carbanion of chloromethyl p-tolyl sulfoxides with ketones at low temperature afforded adducts in almost quantitative yields, which were exposed to t-BuOK to give sulfinyloxiranes in high yields. The sulfinyloxirane was reacted with benzylamine to give α-amino al...
Aggregation of α-synuclein (α-Syn) play a key role in the development of Parkinson Disease (PD). One of the effective approaches is to stabilize the native, monomeric protein with suitable molecule ligands. We have designed and synthesized a series of sheet-like conjugated compounds which poss...
Direct and efficient α-fluorination of amides—which are ubiquitous in natural products, pharmaceuticals, and organic materials—remains a long-standing challenging task. In a recent paper in Nature Chemistry, Maulide and colleagues described a direct and chemoselective nucleophilic α-fluorina...
A series of chiral propargylic alcohols with high enantiomeric excess was prepared by asymmetric dihydroxylation of α,β-unsaturated esters, conversion of the diols to 4-(chloromethyl)-1,3-dioxolane intermediates, and base-induced elimination.
β-Enamino esters or amides can be synthesized in a single step by a carbonylative coupling of α-chloroimines with alcohols or amines under Pd-catalysis. The methodology has been also applied to the preparation of heteroaryl acetic acid derivatives starting from chloromethyl heteroaromatic ring...
Improvement of subtype selectivity of an inhibitor’s binding activity using the conformational restriction approach has become an effective strategy in drug discovery. In this study, we applied this approach to PDE4 inhibitors and designed a series of novel oxazolidinone-fused 1,2,3,4-tetrahydr...
Benzoxazoles 2 can be smoothly synthesized by treatment of starting materials of N-(2-hydroxyaryl) cyclopropyl amides 1 with PPh3/CCl4 in acetonitrile in good yields. When PPh3/CBr4/MS 4 Å was used in the reaction system, the corresponding ring-expanding products 3 were obtained in moderate to g...
A new series of (E)-1-(4-substituted)-3-(4-hydroxy-3-nitrophenyl) prop-2-en-1-one compounds have been synthesized by Claisen–Schmidt condensation reaction. Nonlinear optical characterization were carried out using z-scan technique with nanosecond pulses. These samples are found to exhibit stron...
ObjectiveExposure to lethal doses of radiation has severe effects on normal tissues. Exposed individuals experience a plethora of symptoms in different organ systems including the gastrointestinal (GI) tract, summarized as Acute Radiation Syndrome (ARS). There are currently no approved drugs for...
A series of 7H-pyrrolo[2,3-d]pyrimidine derivatives were designed and synthesized as reversible BTK inhibitors, and evaluated their kinase selectivity, anti-proliferation against the B-cell lymphoma cell lines (Ramos, Jeko-1) and cell line BTK enhanced (Daudi) in vitro. Among them, compound 28a ...
We describe the identification of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine (3), a potent, orally active Src inhibitor with desirable PK properties, demonstrated activity in human tumor cell lines and in animal models of tumor growth.
Novel photochromic benzimidazol[1,2a]pyrrolidin-2-ones, which give thermally stable highly coloured photochromes, have been synthesised by condensation of 2-methyl-3-benzothienylethylidene(isopropylidene)succinic anhydride with 1,2-diaminobenzene and its 4,5-dimethyl and 4,5-dimethoxy derivative...
A series of 6-substituted 3-(pyrrolidin-1-ylmethyl)chromen-2-ones (coumarins) have been synthesized and their inhibitory activity to human monoamine oxidase A (MAO A) and B (MAO B) determined. Incorporation of a basic amino function in the C3 position together with substitution at the C6 positio...
2-(3-Alkylaminophenyl)-6-(pyrrolidin-1-yl)quinolin-4-ones 1–3 were synthesized and screened for anti-proliferative activity against three human cancer cell lines, as well as the normal cell line Detroit 551. All of the synthesized target compounds 1–3 demonstrated potent cytotoxic activity aga...
Thiocyanate-selective electrodes based on nickel and iron phthalocyanines are described. The electrodes were prepared by incorporating the ionophores into plastisized poly(vinyl chloride) membranes, which were directly coated on the surface of graphite electrodes. The resulting electrodes demons...
An ELM process using tri-noctylphosphine oxide (TOPO) to extract cobalt from the zinc plant acidic thiocyanate leach solutions containing cobalt and nickel has been presented. ELM consists of a diluent (kerosene), a surfactant (SPAN 80), and a carrier (TOPO). 6 M NH3 solution has been used as st...
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