A protocol of [3 + 3]-cycloaddition was proposed for the synthesis of 2H-1,4-thiazin-3(4H)-ones and thiomorpholine-3,5-diones from α-chlorohydroxamates and 1,4-dithiane-2,5-diol. This direct and practical method provides a novel and rapid approach for the synthesis of thiomorpholin-3-one deriva...
We report a novel series of quinoxaline derivatives from which agents with antiproliferative activity have been identified. Two ethyl 3-(arylethynyl)quinoxaline-2-carboxylates demonstrated substantial antiproliferative activity against both human non-small cell lung carcinoma (A549) and glioblas...
Fluorescent ethyl 3-phenothiazinyl propiolates with reversible Nernstian oxidation potentials were efficiently synthesized by an improved Sonogashira coupling of aryl iodides and ethyl propiolate. The versatility of this modified alkynylation was illustrated by 13 ethyl 3-arylpropiolates in most...
Ethyl (Z)-2-fluoropropenoate reacts stereospecifically and regioselectively in [3 + 2] cycloadditions with aryl N-methylnitrones. The yields of the cycloaddition products range from 61 to 70%.
An inclusive study towards the stereospecific synthesis of novel cis-3-monosubstituted-β-lactams from cis-3-functionalized 3-phenylsulfonyl/sulfinyl-β-lactams is described. 3-Sulfinyl-β-lactams 5/5ʹ successfully furnished stereospecific cis-3-monosubstituted-β-lactams 6, however 3-sulfonyl-β...
3-Methylmethcathinone (3-MMC or metaphedrone) is a synthetic cathinone, recently introduced in the market of the new psychoactive substances (NPS), initially to replace mephedrone (4-methylmethcathinone or 4-MMC), and rapidly widespread among drug users. 3-Methylmethcathinone is legally controll...
We present a theoretical study of the structure and electronic and optical properties of several L2–M compounds where L is bis(N-(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)ethanimidamidato, or C11H11N4O2, and M = Co, Ni, Cu, Zn, Pd, Cd. Our calculations are carried out in the framework of the de...
A protocol of [3 + 3]-cycloaddition was proposed for the synthesis of 2H-1,4-thiazin-3(4H)-ones and thiomorpholine-3,5-diones from α-chlorohydroxamates and 1,4-dithiane-2,5-diol. This direct and practical method provides a novel and rapid approach for the synthesis of thiomorpholin-3-one deriva...
This chapter is the review of developments in the physical properties, synthesis, and applications of fused bicyclic, tricyclic, and polycyclic azetes, azetines, and azetidines in the last decade. A noticeable feature is the increased number of fused rings in the compounds reported and hence the...
2-Cyano azetidines, easily accessible from β-amino alcohols, are precursors of stereodefined homochiral azetidinic or pyrrolidinic 1,2-diamines. A small library of these original diamines was screened as precatalysts for the enantioselective addition of 1,3-dicarbonyl compounds onto β-nitro st...
The four-membered azaheterocycles, azetidines and azetidin-2-ones are thermally stable and easy to handle. Structures of many compounds have been established by X-ray crystallography.Azetidines react with electrophiles and nucleophiles. The ring opening affords useful amides, alkenes, and amines...
Oxetane-benzopyran spirocycles were synthesised via a palladium catalysed cyclisation-cross coupling cascade reaction whilst oxetane/azetidine-pyrrolidino isoindolone spirocycles were synthesised via a silver catalysed 1,3-dipolar cycloaddition reaction followed by a palladium catalysed carbonyl...
The present study was undertaken to evaluate in-vivo hypolipidemic activity of a novel series of 2-methyl-2-(substituted phenyl isoxazol)phenoxyacetic acid derivatives by triton induced hyperlipidemia in rats. The newly synthesized compounds 5a, 5d and 5g showed significant decrease in the serum...
A series of metal-free novel organic dyes MR1, MR2, MR3 and MR4 containing N, N-diethylaniline as a donor group, rhodanine-3-acetic acid as an acceptor group separated by thiophene as a spacer were designed and synthesized. The detailed study of electrochemical, photophysical, photovoltaic and t...
New complexes of dl-piperidine-2-carboxylic acid (dl-H2pa), [Zn(Hpa)(AcO)(H2O)2], trans-[Zn2(μ-Ca)2(Hpa)2Cl6], [M(bpy)(Hpa)]Cl and [M(pa)(PPh3)2] (M(II) = Pd, Pt) have been prepared and characterized on the basis of elemental analyses, molar conductivity and thermal measurements, IR, Raman, UV–...
An efficient ionic liquid system was developed for the preparation of various heterocycle-fused pyrimidine-2, 4(1H,3H)-diones in moderate to excellent yields (52–95%). It was found that [HDBN+][TFE−], a simple and easily prepared ionic liquid, could act as both the solvent and reaction promoter...
A facile one-pot synthesis of new 3-arylthieno[2,3-d]pyrimidine-2,4(1H,3H)-diones via base-catalyzed cyclocondensation of ethyl 2-amino-4,5-dimethylthiophene-3-carboxylate with aryl isocyanates is described.
Checkpoint kinase 1 (CHK1) inhibitors can potentiate the effectiveness of deoxyribonucleic acid (DNA) damaging agents in the treatment of cancer. A novel series of 2,6-disubstituted-9H-purine (3a-p, 5a and 5b), 2,4-disubstituted-thieno[3,2-d]pyrimidine (8a-c) and 2,4-disbustituted-7H-pyrrolo[2,3...
A series of novel five-membered heteroaromatic ring fused-pyrimidine derivatives including purines, pyrrolo[2,3-d]pyrimidines, pyrrolo[3,2-d]pyrimidines, thieno[2,3-d]pyrimidines, thieno[3,2-d]pyrimidines and furo[3,2-d]pyrimidines have been identified to be potent inhibitors of hedgehog signali...
In light of the emergence of resistance against the currently available EGFR inhibitors, our study focuses on tackling this problem through the development of dual EGFR/HER2 inhibitors with improved enzymatic affinities. Guided by the binding mode of the marketed dual EGFR/HER2 inhibitor, Lapati...
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