A synthetic access to photochromic spirooxazines is developed through the condensation of methylene-substituted azaheterocycles on 1-amino-2-naphthols in presence of an oxidizing agent. Compared to usual preparation of this kind of compounds (via 1-nitroso-2-naphthols), yields are generally good...
A series of N-phenyl- and N-benzyl-2-azaspiro[4.4]nonane- and [4.5]decane-1,3-diones containing a fluoro or trifluoromethyl substituents at the aryl ring was synthesized and tested for their anticonvulsant activity in the maximal electroshock (MES) and subcutaneous metrazole (sc.Met) tests. Amon...
To continue our systematic SAR studies, two series of N-benzyl- (X = CH2) and N-aminophenyl- (X = NH) derivatives of 2-azaspiro[4.4]nonane (1a–1j) and 2-azaspiro[4.5]decane-1,3-dione (2a–2j) were synthesized, and evaluated in maximum electroshock seizure (MES), subcutaneous pentylenetetrazole ...
The synthesis, physicochemical and pharmacological properties of new N-phenylamino derivatives of 2-azaspiro[4.4]nonane-1,3-dione (8–10), 2-azaspiro[4.5]decane-1,3-dione (11–18) and 3-cyclohexyl-pyrrolidine-2,5-dione (19, 20) derivatives were described. The anticonvulsant properties of those c...
An in-depth study of the reactions of 4-(ethynyl)-4-hydroxy-2,3-substituted-2-cyclobuten-1-ones with N-bromo- or N-iodosuccinimide, affording in most cases 2-halomethylene-4-cyclopentene-1,3-dione, is described. This reaction was used in a short total synthesis of methyl linderone.
Contraction and electrophysiological effects of 5-methylfurmethiodide (MFI), a selective muscarinic agonist in mammals, were tested on Ascaris suum muscle strips. In a contraction assay, MFI produced weak contraction and was less potent than levamisole and acetylcholine. Atropine (3 μM) a non-s...
A four-component reaction between 2-formylbenzoic acid, malononitrile, isocyanides, and primary alkyl amines has been developed for an efficient preparation of 2-(1-(alkylcarbamoyl)-2,2-dicyanoethyl)-N-alkylbenzamide and 1,7-diazaspiro[4,4]nonane-2,6-dione derivatives under two different conditi...
A novel one-pot isocyanide-based cascade four-component reaction between primary alkylamines, acetylenic esters, and alkyl isocyanides led to tetraalkyl 1-alkyl(aryl)-4-alkylamino-1,2-dihydropyridine-2,3,5,6-tetracarbxylates in good yields.
The multicomponent Ugi reaction is a straightforward method that can be used for the synthesis of highly hindered C-tetrasubstituted amino acids by reacting an amine, a ketone or aldehyde, a carboxylic acid and an isocyanide. In the present work, the synthesis of several α,α-dialkylglycines (α...
A simple impedimetric label-free immunosensor was developed for the specific and sensitive detection of mucin 4 (MUC 4) protein by using graphite based screen printed electrodes modified with an aryl diazonium salt or compound (p- aminophenylacetic acid) for the immobilization of antibody anti-M...
A synthetic approach to the butyrolactones of (2SR,4SR)-5(S)-(N-Boc)-amino-6-cyclohexyl-4-hydroxy-2-isopropyl hexanoic acid from (L)-phenylalanine and the preparation of the n-butyl amide of the 2(S),4(S),5(S) acid is presented.
A new enantioselective synthesis of a valuable hydroxyethylene dipeptide isostere precursor, (4S, 5S)-5-5(N-Boc)-amino-6-cyclohexyl-4-hydroxy-hexanoic acid lactone, has been developed by using coupling reaction of chiral triflates as a key step.
Simple and precise high-performance liquid chromatographic (HPLC) assays were developed and validated for the determination of a renin inhibitor (RI), 4-cyclohexyl-2-hydroxy-3-(3-methylsulfanyl-2-{2-[(morphine-4-carbonyl)amino]- 3-phenylpropionylamino}propionylamino)butyric acid isopropyl ester ...
A stereoselective synthesis of the hydroxyethylene dipeptide isostere, (2S,4S,5S)-5-amino-6-cyclohexyl-4-hydroxy-2-isopropyl hexanoic acid n-butyl amide from Boc-L-phenylalanine is described.
The TiCl4-mediated formal [3+3] cyclocondensation of 1,3-bis(trimethylsilyloxy)-1,3-butadienes with 1,1-dimethoxy-4,4-dichlorobut-1-en-3-one afforded a variety of functionalized 6-dichloromethyl-4-methoxysalicylates with very good regioselectivity. Some of the products were transformed into 6-fo...
The influence of humic acid (HA) on U(VI) sequestration by calcium titanate (CaTiO3) was investigated by batch experiment and spectroscopic techniques. Various characterizations, including zeta potentials, average hydrodynamic diameters, specific surface area and pore volume, have been demonstra...
Aligned Ag nanorod arrays prepared by oblique angle vapor deposition (OAD) were utilized to observe the SERS response for cast films of adsorbed uranyl ion complexes. These nanorod arrays consisted of preferentially aligned and tilted cylindrically shaped nanorods (average nanorod length = 858 n...
In the present work, we reported the preparation of a highly porous phosphate-functionalized graphene (HGP) hydrogel electrode material by a two-step process for uranium (U(VI)) electrosorption. The extra pores were pre-created on graphene nanosheets by a simple H2O2 etching reaction, and then t...
The novel [email protected] was utilized as a promising adsorbent for the adsorption and separation of U(VI) ions from aqueous solutions for the first time. The material performed potential adsorption capacity of 292.2 mg g−1 and an outstanding selectivity on U(VI) at pH = 4.5. Furthermore, the ...
The development of photocatalysts active under visible light attracts great attention due to the prospect for the utilization of solar radiation. The modification of porous supports with uranyl ions results in the ability for oxidation of organic compounds under visible light up to 500 nm in wav...
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