Reductive alkylation of thioureas: a highly practical synthesis of unsymmetrical N,N′-disubstituted thioureas

A highly practical synthesis of unsymmetrical N,N′-disubstituted thioureas by the reductive alkylation of N-monosubstituted thioureas with aldehydes is described. N-Monosubstituted thioureas can in turn be synthesized by the reductive amination of thiourea with an appropriate aldehyde. This reductive alkylation methodology was also extended to carbamates.     

OPTIMIZATION OF MULTIFIBER LIGHT DELIVERY FOR THE PHOTODYNAMIC THERAPY OF LOCALIZED PROSTATE CANCER

The understanding of light distribution within the target organ is essential in ensuring efficacy and safety in photodynamic therapy (PDT). A computer simulator of light distribution in prostatic tissue was employed for optimizing dosimetry for PDT in localized prostatic cancer. The program was based on empirically determined light distributions and optical constants and an assumed Ruence rate differential from fiber source to necrosis periphery. The diffusion theory approximation to the Boltzmann transport equation was the applicable formulation relevant to prostatic tissue, which has a high albedo with forward-scattering characteristics. Solving this equation of diffusive transfer for the appropriate fiber geometry yielded the energy fluence distributions for cleaved fiber and cylindrical diffuser light delivery. These distributions, confirmed by our measurements, show a l/r and l/r dependency (r = distance from light source) of the fluence ø(r) for the cleaved fiber and diffuser, respectively. This manifests itself by the tighter spacing of energy fluence isodoses in the case of the cleaved fiber. It was predicted that for a typical PDT regime a single interstitially placed cleaved fiber would treat 0.05–0.72 cm³, Four parallel fibers improve the uniformity of light distribution and treatment volume, and an interfiber separation of 12 mm would be necessary to provide optimal overlap of PDT necrosis, treating 0.26–3.6 cm³. The cylindrical diffuser, however, could treat larger volumes, and it was predicted that four 3 cm long diffusers at an optimal separation of 25 mm would treat 25–88 cm³ of prostatic tissue.     

A General and Facile Synthesis of l,3-Diaryl-4-pyrazoleacetic Acids and Its Application in the Synthesis of SDZ RGU 825

1,3-Diaryl-4-pyrazoleacetic acids and derivatives exhibit multiple biological activities.¹ For example, Lonazolac^® is listed in Merck index as an antiinflammatory and analgesic agent. We were interested in this type of compounds for their potential applications in anti-diabetics. One of the leading candidates, SDZ RGU 825,has been shown to enhance whole-body glucose disposal without increasing insulin secretion. Therefore, it was developed for treatment of "non-insulin-dependent diabetes mellitus",the type Ⅱ diabetics.     

Deprotection of heteroaromatic carbamates via a base-catalyzed methanolysis

A simple and mild method for the deprotection of heteroaromatic carbamates via methanolysis using a catalytic amount of base such as sodium methoxide, DBU, or Verkade’s base (proazaphosphatranes) is presented. Carbamate protecting group of an aliphatic amine is not affected under these conditions.     

The photosensitized rearrangement of aryl-substituted tricyclo[2.2.0.02,6]hexanes to bicyclo[3.1.0]hex-2-enes

The triplet sensitized irradiation of 3-allyl-diaryl-substituted cyclopropenes to bicyclo[3.1.0]hex-2-enes proceeds via an intramolecular [2+2]-cycloaddition followed by a subsequent rearrangement of the initially formed tricyclo[2.2.0.0^2,6]hexane skeleton.     

A general and facile synthesis of 1,3‐diaryl‐4‐pyrazoleacetic acid esters

A general synthesis of 1,3‐diaryl‐4‐pyrazoleacetic acid esters has been realized via the condensation of a γ‐carboxy ester hydrazone with the Vilsmeier reagent.     

THE UPTAKE OF PORPHYRIN AND ZINC-METALLOPORPHYRIN BY THE PRIMATE PROSTATE

Abstract— The relative distribution of sensitizer drugs in the prostate and its contiguous organs is of importance in the treatment of localized prostatic cancer with photodynamic therapy. Using the primate model, whose prostate is both morphologically and physiologically homologous with its human counterpart, the distribution of hematoporphyrin derivative (HpD) amongst organs of urological interest was determined. Hematoporphyrin derivative levels were comparatively low in both caudal and cranial prostatic lobes (0.93-1.77 μg/g) and were similar to those in rectum, urethra and the skin. The reticuloendothelial organs, liver, spleen and also the kidney accumulated the highest quantities of porphyrin (4.76-9.8 μg/g, liver > spleen > kidney). Despite a high avidity of prostatic tissue for zinc, a zinc-metalloporphyrin (Zn-HpD) did not concentrate selectively in the prostate. The results are of clinical value in view of the homology between the primate and the human.     

Generating virtual textile composite specimens using statistical data from micro-computed tomography: 1D tow representations for the Binary Model

A Monte Carlo algorithm is defined for generating replicas of textile composite specimens that possess the same statistical characteristics as specimens imaged using high resolution computed tomography. The textile reinforcement is represented by one-dimensional tow loci in three-dimensional space, which are easily incorporated into the Binary Model of textile composites. A tow locus is expressed as the sum of non-stochastic, periodic variations in the coordinates of the tow centroid and stochastic, non-periodic deviations. The non-stochastic variations have period commensurate with the dimensions of the unit cell of the textile, while the stochastic deviations, which describe geometrical defects, exhibit correlation lengths that may be incommensurate with the unit cell. The model is calibrated with data deduced in prior work from computed tomography images. The calibration obviates the need for assuming any ideal shape functions for the tow loci, which can take very general form. The approach is therefore valid for a wide range of textile architectures. Once calibrated, a Markov Chain algorithm can generate numerous stochastic replicas of a textile architecture very rapidly. These virtual specimens can be much larger than the real specimens from which the data were originally gathered, a necessary feature when real specimen size is limited by the nature of high resolution computed tomography. The virtual specimen generator is illustrated using data for an angle interlock weave.     

An efficient and practical N-methylation of amino acid derivatives

[reaction: see text] An efficient and practical N-methylation of amino acid derivatives with dimethyl sulfate in the presence of sodium hydride and a catalytic amount of water is described. Reaction of water with sodium hydride generated highly reactive dry sodium hydroxide, which led to much faster reaction rates than powdered sodium hydroxide itself.