Polycyclic aromatic hydrocarbons (PAHs) are a group of persistent organic compounds. White rot fungi (WRF) have attracted much attention due to their strong capabilities for the initial transformation of PAHs. To better understand the metabolic pathway of PAHS by WRF in the presence of ligninoly...
[3+2]-Photocycloaddition of di-(−)-menthyl, di-(−)-8-phenylmenthyl, and di-(−)-bornyl 1,4-naphthalenedicarboxylates to alkenes, such as isobutene, styrene, and α-methylstyrene, proceeded with diastereoselectivity, up to 62% diastereomeric excess (de), largely depending on the concavity of the a...
Amino acids may be used as coupling partners for esterification with 3-hydroxy glycals as substrates for the tandem Tebbe/Claisen approach to the synthesis of C-glycosyl amino acids. Whilst esters of substituted α-amino acids do not successfully undergo Tebbe, or other, methylenation, esters of...
The first total synthesis of benzonaphthyridine alkaloid (1), a unique diazaphenathrene alkaloid isolated from mangrove-derived Streptomyces albogriseolus, was accomplished. The core structure was unequivocally constructed via several key transformations, such as Knoevenagel condensation, Curtiu...
Novel diorganotin(IV) derivatives of l-Arginine (HArg), Nα-(tert-Butoxycarbonyl)-l-Arginine (Boc–Arg–OH) and l-Ala-l-Arg (H2Ala–Arg), H2NC(NH)NH(CH2)3CH(NHR′)CO2H, where R′ = H in HArg, R′ = C(O)OC(CH3)3 in Boc–Arg–OH, R′ = H2NCH(CH3)CO in H2Ala–Arg and triorganotin(IV) derivatives of...
A new approach to synthesize ‘carba’ Ψ[CH2CH2] dipeptides, e.g. Boc-d-Phe-Ψ[CH2CH2]-l-Arg(NO2)-OH and Boc-d-Phe-Ψ[CH2CH2]-d-Arg(NO2)-OH, is described.
A series of mono- and disubstituted O-ferrocenoyl conjugates of 3-trans- and 4-trans-hydroxy-L-proline amino acids are synthesized. These conjugates are protected by tert-butloxycarbonyl (Boc) group at the N-terminus. The Boc removal of the ferrocene (Fc) hydroxy-L-proline conjugates affords a s...
The synthesis of several A and AE ring analogues of the alkaloid methyllycaconitine is reported. The key 2-(2″-methylsuccinimido)benzoate ester pharmacophore is introduced using an efficient two step procedure. Esterification of the alcohol precursors with N-(trifluoroacetyl)anthranilic acid un...
Androgen receptor (AR) antagonists are used for hormone therapy of prostate cancer (PCa). However resistance to the treatment occurs eventually. One possible reason is the occurrence of AR mutations that prevent inhibition of AR-mediated transactivation by antagonists. To offer in future more op...
The amino acid-conjugates (1a–k) with eleven amino acids attached to primary amine of (S)-1-[1-(4-aminobenzoyl)-2,3-dihydro-1H-indol-6-sulfonyl]-4-phenyl-imidazolidin-2-one (DW2282, 1) were prepared and studied for their prodrug characteristics and anti-cancer activity against SW620 cell line. ...
The kinetics of the pH-independent hydrolysis of 4-methoxyphenyl dichloroacetate were investigated with and without ultrasonic irradiation in acetonitrile–water binary mixtures containing 0.008 to 35 wt.% of acetonitrile and the kinetic sonication effects (kson/knon) were calculated. Molecular ...
The methylenecyclopropanes 1 react with LiCl, LiBr or NaI at 80 °C to give the corresponding gem-disubstituted homoallylic halides 2 in good to excellent yields in acetic acid. In some cases, the ring-opening reaction can be completed within 5 min to give the corresponding gem-disubstituted hom...
An efficient solvent-free protocol for the synthesis of 14-aryl-14H-dibenzo[a,j]xanthenes from the condensation of 2-naphthol with arylaldehydes, using acetic acid functionalized imidazolium salts (1-carboxymethyl-3-methylimidazolium bromide ([cmmim]Br) and 1-carboxymethy1-3-methylimidazolium te...
With an intention to synergize the anti-bacterial activity of chalcones and rhodanine-3-acetic acid, several hybrid compounds possessing chalcone and rhodanine-3-acetic acid moieties were synthesized and tested for their anti-bacterial activity. Some compounds presented great anti-microbial acti...
A library of fourteen 2-imino-4-thiazolidinone derivatives (1a-1n) has been synthesized and evaluated for in vivo anti-inflammatory activity and effect on ex-vivo COX-2 and TNF–α expression. Compounds 1k (5-(2,4-dichloro-phenooxy)-acetic acid (3-benzyl-4-oxo-thiazolidin-2-ylidene)-hydrazide) a...
A series of new (2,4-dioxothiazolidin-5-yl/ylidene)acetic acid derivatives with thiazolidine-2,4-dione, rhodanine and 2-thiohydantoin moiety (28–65) were synthesized by the reaction of (2,4-dioxothiazolidin-5-yl/ylidene)acetic acid chlorides with 5-(hydroxybenzylidene) thiazolidine-2,4-dione, r...
The relative thermal and oxidative stabilities of N-[3-(triethoxysilyl)propyl]2,4-dinitroaniline (1), incorporated covalently into sol-gel coatings and of 2,4-dinitroaniline, incorporated non-covalently into similar coatings, showed no significant difference in relative thermal stability in sol-...
A simple and rapid method is described for chromatographing mono- and bis-2,4-dinitrophenylhydrazones derived from hydroxycarbonyl compounds. The derivatives were separated by the thin-layer technique on aluminium oxide or silica gel plates with toluene-ethyl acetate mixtures as solvents. Sprayi...
The separation of 41 mono-, bis-, and tris-2,4-dinitrophenylhydrazones derived from simple saturated aldehydes and ketones, unsaturated aldehydes, di-, tri-, and hydroxycarbonyl compounds, and α-ketoacids by thin-layer chromatography is described. The cis- and trans-isomers of some of these com...
The reaction between R3SbCl2 (R = Me, Ph) and R′2PO2Na (R′ = Me, Ph) afforded R3Sb(O2PR′2)2 derivatives, which were investigated by IR and multinuclear (1H, 13C, 31P) NMR spectroscopy. Attempts to grow crystals of Me3Sb(O2PPh2)2 led to colorless needles identified by X-ray diffractometry as M...
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