ortho‐Benzoxylation of N‐Alkyl Benzamides with Aromatic Acids Catalyzed by Ruthenium(II) Complex

A highly regioselective ortho‐benzoxylation of N‐alkyl benzamides with aromatic acids in the presence of [{RuCl₂(p‐cymene)}₂], AgSbF₆, and (NH₄)₂S₂O₈ in 1,2‐dichloroethane at 100 °C for 24 h affording ortho‐benzoxylated N‐alkyl benzamides by C?H bond activation is described. Further, Ru‐catalyzed alkenylation is done at the ortho C?H bond of benzoxylated N‐alkyl benzamides with alkenes in water solvent. Subsequently, the benzoxyl moiety of N‐alkyl benzamides was converted into a hydroxyl group in the presence of base or acid. A possible reaction mechanism was proposed to account for the present coupling reaction.     

Simulation and experimental studies of a vibro-impact capsule system driven by an external magnetic field

This paper studies the electromagnetic field used for driving a vibro-impact capsule prototype for small bowel endoscopy. Mathematical models of the electromagnetic field and the capsule system are introduced, and analytical solution of the magnetic force applied on the capsule is derived and verified by experiment. The impact force between the inner mass of the capsule and the capsule body is also compared via numerical simulation and experimental testing. By comparing the capsule’s progressions under different control parameters (e.g. the excitation frequency and duty cycle), the merits of using the vibro-impact propulsion are revealed. Based on the experimental results, the optimised speed of the prototype can achieve up to 3.85 mm/s. It is therefore that the potential feasibility of using the external electromagnetic field for propelling the vibro-impact capsule system is validated.

     

Simultaneous Trace Level Determination of Potentially Genotoxic Hydrazine,Methylhydrazine and Alkylamines in Pharmaceutical Substances by CE Using Indirect Photometric Detection

A simple, fast, and sensitive capillary electrophoretic method was developed for determining two genotoxic impurities hydrazine and methylhydrazine and eight alkyl amines at trace levels in pharmaceutical substances using indirect photometric detection. The method development involved a systematic screening of various cationic visualizing reagents and optimization of separation conditions to obtain the best resolution and sensitivities. The optimized method was validated for specificity, precision, linearity, and accuracy. Linear calibration curves (R > 0.99) were obtained for all analytes in the range LOQ–200 % of nominal concentrations. The developed CE method was effectively implemented for estimating hydrazine and alkylamines in several active pharmaceutical ingredients (APIs).

     

Embedding ω-continuous posets in function spaces of domains

We prove a number of results, including the following: IfD is an ω-algebraic poset which is not an antichain, andE is an ω-continuous poset, then there exists a Scott-continuous order-embedding fromE to [D?D]; in particular, there exists a Scott-continuous order-embedding from (P(ω), ⊂-) to [D?D]. The proof of this main result does not use the Axiom of Choice.     

A convenient protocol for C-H oxidation mediated by an azido radical culminating in Ritter-type amidation

Cerium(IV) ammonium nitrate in combination with sodium azide reacts with unactivated hydrocarbons in acetonitrile to furnish acetamides in one pot. The strategy can be used to introduce nitrogen functionality into a variety of compounds; a carboxylic ester directly afforded the corresponding α-amino acid.     

Neutron emission from a 100 joule plasma focus

A neutron yield of } 5×10⁵ D-D neutrons/discharge was obtained when 0.1 KJ of energy was pumped into a plasma focus of Mather type. The neutron yield was measured by a high sensitivity silver activation counter. The results are compared with those of other laboratories and it is found that neutron yield scales asE ^1.73 orI ^4.29 in the 0.1–500 KJ region.     

Stereoselective functionalisation of SuperQuat enamides: asymmetric synthesis of homochiral 1,2-diols and α-benzyloxy carbonyl compounds

Homochiral (E)- and (Z)-enamides derived from SuperQuat (S)-4-phenyl-5,5-dimethyl-oxazolidin-2-one undergo highly diastereoselective epoxidation upon treatment with dimethyldioxirane. Subsequent epoxide opening with meta-chlorobenzoic acid proceeds via a stereoselective S_N1-type process, with retention of configuration, to give the corresponding 1′-m-chlorobenzoyl-2′-hydroxy derivatives. Treatment of the SuperQuat enamides with mCPBA effects this two-step transformation in one pot. Reductive cleavage of the isolated 1′-m-chlorobenzoyl-2′-hydroxy derivatives (≥96% de) generates homochiral 1,2-diols in ≥96% ee. Alternatively, regioselective lithiation of the enamide at C(1′) with ^tBuLi followed by reaction with an aromatic aldehyde and in situ O-benzylation generates a 1′-(benzyloxy-aryl-methyl) substituted enamide with high diastereoselectivity. Subsequent oxidative cleavage of the enamide CC bond with NaIO₄/RuCl₃ followed by methanolysis of the resultant N-acyl fragment furnishes an O-benzyl protected α-hydroxy methyl ester in high ee.