A facile approach to phosphonic acid diesters

The symmetric H‐phosphonates of carbohydrate and other compounds were conveniently prepared by direct transesterification of the corresponding monohydroxylic compounds with diphenyl phosphite. The approach has the merits of mild reaction conditions and high yields. © 2003 Wiley Periodicals, Inc. Heteroatom Chem 14:208–210, 2003; Published online in Wiley InterScience (www.interscience.wiley.com). DOI 10.1002/hc.10130     

Make conjugation simple: a facile approach to integrated nanostructures

We report a facile approach to the conjugation of protein-encapsulated gold fluorescent nanoclusters to the iron oxide nanoparticles through catechol reaction. This method eliminates the use of chemical linkers and can be readily extended to the conjugation of biological molecules and other nanomaterials onto nanoparticle surfaces. The key to the success was producing water-soluble iron oxide nanoparticles with active catechol groups. Further, advanced electron microscopy analysis of the integrated gold nanoclusters and iron oxide nanoparticles provided direct evidence of the presence of a single fluorescent nanocluster per protein template. Interestingly, the integrated nanoparticles exhibited enhanced fluorescent emission in biological media. These studies will provide significantly practical value in chemical conjugation, the development of multifunctional nanostructures, and exploration of multifunctional nanoparticles for biological applications.     

A facile approach to hexagonal ZnO nanorod assembly

Nanocrystalline ZnO nanorods were successfully grown by ultrasonication using an acidic ethanolic zinc acetate precursor solution followed by a flow coating process and annealing at 600 °C. The ZnO nanorods obtained were hexagonal in shape and showed a high degree of uniformity in size and distribution. These samples were characterized by X-ray diffraction (XRD), energy dispersive X-ray (EDX) spectroscopy, X-ray photoelectron spectroscopy (XPS), scanning electron microscopy (SEM) and Raman spectrophotometry and the results are discussed. This approach appears to be the easiest way to fabricate bulk ZnO nanorods.     

First stereoselective total synthesis of Neocosmosin A: a facile approach

First stereoselective concise synthesis of Neocosmosin A, with in vitro binding affinity for human opioid and cannabinoid receptors, has been reported using readily available starting materials such as methylacetoacetate, cyclohexanone, and homoallyl alcohol involved in the key transformations. There are three fragments involved in the synthesis of target molecule, bearing acid functionality, (R)-pent-4-en-2-ol, and Weinreb amide which are synthesized in four, eight, and three steps, respectively. Then the fragments were coupled in four steps to yield the target molecule in an overall yield of 28.6%.     

A new facile approach to N-alkylpyrroles from direct redox reaction of 4-hydroxy-l-proline with aldehydes

An unprecedented acetic acid-catalyzed efficient access to N-alkylpyrroles from reaction of 4-hydroxy-L-proline with a variety of aldehydes has been achieved in good to excellent yields under mild reaction conditions.     

A facile two-step high yield approach to 2-oxasteroids

The base catalyzed autoxidation of 3-oxo-Δ⁴ steroids in aprotic media at circa -25°C occurs nearly exclusively at C₂ of the A-ring, generating rapidly (< 4 hrs) and in high yield the corresponding enol (2-hydroxy-3-oxo-Δ^1,4 analog) When the reaction is then allowed to continue at room temperature for several days, the enol is further autoxidized to the related lactol (1-hydroxy-2-oxa-3-oxo-Δ⁴ analog) in overall yields generally in the range of 85–95%. Sodium borohydride reduction of the lactol yields the pharmacologically important 2-oxasteroids.     

A facile two synthon approach to the camptothecin skeleton

A synthesis of deethyldesoxycamptothecin via the reaction of two readily accessible synthons is described. One of the synthons constitutes the ABC ring system of camptothecin, while the second provides all the C atoms of the rings D and E. The synthetic approach is suited for the total synthesis of camptothecin analogues.     

A facile conversion of ethoxydihydropyrans to 4-cyanoethylisoxazoles

The reaction of ethoxydihydropyrans 2 , which were prepared from 2-methylene-1,3-dicarbonyl compounds 1 with ethyl vinyl ether, and hydroxylamine hydrochloride gave 4-cyanoethylisoxazoles 3 whose substituents at the 3 and 5 positions were transformed from substituent at the 2 position and the acyl group of 2 regioselectively.     

A new approach to the facile synthesis of 2-substituted-quinazolin-4(3H)-ones

A new approach to the facile synthesis of 2-substituted-quinazolin-4(3H)-ones and its derivatives using the condensation reaction of substituted 2-aminobenzamide and orthoesters is reported.     

A new synthetic approach to the lactol moiety of halichoblelide

A stereoselective approach to the γ-lactol moiety of halichoblelide is described starting from commercially available (R)-3-butyn-2-ol. The key step is the hydroboration of a chiral protected 1,2-butadien-3-ol and its addition to furfural.     

A facile and highly atom-economic approach to biaryl-containing medium-ring bislactones

Starting from readily available phenanthrenequinone and alkenes, biaryl containing medium-ring bislactones could be easily prepared through sequential photocycloaddition-photooxidation reactions with good yields and diastereoselectivity.     

A facile approach to fabricate functionalized superparamagnetic copolymer-silica nanocomposite spheres

Novel amino- or thiol-functionalized superparamagnetic copolymer-silica nanospheres (NH(2)-SMCSNs/SH-SMCSNs), which consist of a magnetic core and a silica cross-linked block copolymer shell, have been fabricated.     

A facile single-step approach to achieve in situ expanded g-C3N4 for improved photodegradation performance

Improved graphitic carbon nitride (g-C₃N₄) was synthesized through a unique one-step cost-effective technique involving a dynamic gas bubbling phenomenon using ammonium chloride (NH₄Cl) as a bubbling agent. An extensive investigation was carried out to optimize the weight ratio of NH₄Cl and melamine during the thermal pyrolysis process. Here, we report an improved form of g-C₃N₄ namely “expanded g-C₃N₄” with increased interlayer distance and remarkable volume expansion. The surface area of this improved version has notably increased leading to higher photocatalytic efficiency as compared with its counterpart, an synthesized without adding NH₄Cl. Synthesized photocatalyst materials were further used to study the Rhodamine B photodegradation under visible light. It was observed that the expanded g-C₃N₄ showed a 2.4 times higher photodegradation rate than its counterpart and degraded 94% of the dye in just 30 min.     

A facile approach to the synthesis of chiral 2-substituted benzofurans

An effective route to chiral optically active 2-substituted benzofurans directly from carboxylic acids is reported. This procedure, which allows the preparation of alpha-alkyl-2-benzofuranmethanamines from N-protected alpha-amino acids without sensible racemization phenomena, proceeds in good yields under mild conditions with the help of microwave irradiation.     

A facile approach to architecturally defined nanoparticles via intramolecular chain collapse

A novel approach is presented for the controlled intramolecular collapse of linear polymer chains to give well-defined single-molecule nanoparticles whose structure is directly related to the original linear polymer. By employing a combination of living free radical polymerization and benzocyclobutene (BCB) chemistry, nanoparticles can be routinely prepared in multigram quantities with the size being accurately controlled by either the initial degree of polymerization of the linear chain or the level of incorporation of the BCB coupling groups. The latter also allows the cross-link density of the final nanoparticles to be manipulated. In analogy with dendritic macromolecules, a significant reduction of up to 75% in the hydrodynamic volume is observed on going from the starting random coil linear chains to the corresponding nanoparticles. The facile nature of the living free radical process also permits wide variation in monomer selection and functional group incorporation and allows novel macromolecular architectures to be prepared. Furthermore, the use of block copolymers functionalized with benzocyclobutene groups in only one of the blocks gives, after intramolecular collapse, a hybrid architecture in which a single linear polymer chain is attached to the globular nanoparticle.