ABSTRACT
3-(1H-Indol-3-yl)benzofuran-2(3H)-ones were efficiently accessed via polyphosphoric acid-mediated condensation of 3-(2-nitrovinyl)-1H-indoles with phenols.
Subject(s)
Benzofurans , Indoles , PhenolsABSTRACT
The recently discovered [4+1]-spirocyclization of nitroalkenes to indoles provided a convenient new approach to 2-(1H-indol-2-yl)acetonitriles. However, this reaction was complicated by the formation of inert 3-(2-nitroethyl)-1H-indole byproducts. Herein, we offer a workaround this problem that allows for effective transformation of the unwanted byproducts into acetonitrile target molecules.
ABSTRACT
Indolizines and pyrazolo[1,5-a]pyridines were prepared via [3 + 2]-cycloaddition of pyridinium ylides to 1-chloro-2-nitrostyrenes. The synthesized molecules were evaluated for antiproliferative activities against a BE(2)-C neuroblastoma cell line with several compounds decreasing the viability of cancer cells. Indolizine 9db showed higher potency than that of all-trans-retinoic acid, an approved cancer drug. Mechanistically, it was found to inhibit tubulin polymerization and it is thus proposed that the discovered chemistry can be exploited for the development of novel microtubule-targeting anticancer agents.
Subject(s)
Tubulin ModulatorsABSTRACT
Nitroalkanes activated with polyphosphoric acid serve as efficient electrophiles in reactions with various nucleophilic amines. Strategically placed second functionality allows for the design of annulation reactions enabling preparation of various heterocycles. This strategy was employed to develop an innovative synthetic approach towards 3,4-dihydroquinazolines from readily available 2-(aminomethyl)anilines.
ABSTRACT
We report a new method for automated identification and measurement of primary particles within soot aggregates as well as the sizes of the aggregates and discuss its application to high-resolution transmission electron microscope (TEM) images of the aggregates. The image processing algorithm is based on an optimized Hough transform, applied to the external border of the aggregate. This achieves a significant data reduction by decomposing the particle border into fragments, which are assumed to be spheres in the present application, consistent with the known morphology of soot aggregates. Unlike traditional techniques, which are ultimately reliant on manual (human) measurement of a small sample of primary particles from a subset of aggregates, this method gives a direct measurement of the sizes of the aggregates and the size distributions of the primary particles of which they are composed. The current version of the algorithm allows processing of high-resolution TEM images by a conventional laptop computer at a rate of 1-2 ms per aggregate. The results were validated by comparison with manual image processing, and excellent agreement was found.
Subject(s)
Image Processing, Computer-Assisted/methods , Soot/chemistry , Algorithms , Humans , Microscopy, Electron, Transmission , Particle SizeABSTRACT
The problem of light scattering by ice crystal particles whose sizes are essentially larger than the incident wavelength is divided into two parts. First, the scattered field is represented as a set of plane-parallel outgoing beams in the near zone of the particle. Then, in the far zone the scattered field is represented as a result of both diffraction and interference of these beams within the framework of physical optics. A proper ray-tracing algorithm for calculation of the amplitude (Jones) scattering matrix is developed and applied. For large particles, a number of reduced Mueller matrices are introduced and discussed, since the pure Mueller matrix obtained from the Jones matrix becomes a rather cumbersome and quickly oscillating value. Backscattering by hexagonal ice crystals, including polarization properties, is considered in detail.