Utilization of bromine azide to access vicinal-azidobromides from arylidene malononitrile

An efficient and facile approach for tetrachlorosilane as an in situ mediated transformation via a one-pot, synthesis of vicinal bromoazides through the generation of BrN₃ from azidochlorosilane and N-bromosuccinimide in acetonitrile as solvent at ambient temperature is achieved. This catalytic process represents a highly regioselective and high yielding method for the synthesis of 1,2-bromoazides. Thiamine pyrophosphate (TPP) riboswitches regulate essential genes in bacteria by changing conformation upon binding intracellular TPP. Molecular docking studies are conducted to understand the orientation and the interaction of each synthesized molecules with TPP riboswitches. 2016 Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences.     

The origins of multifractality in financial time series and the effect of extreme events

In this paper, we study the impacts of noise and time delay in the monomer-dimer (MD) surface reaction model by using theoretical analysis. The MD models for various dimer adsorption mechanisms (namely, local and random adsorption models), which exhibit the first- and second-order phase transitions (PTs), are analyzed. By comparison with two various dimer adsorption, it is found that the qualitative predictions of the well-known first- and second-order PTs are better for the random adsorption model than that for the local adsorption model. The validity of approximate analytic results is checked by numerical simulations.     

Pyrazolothiazoles: Synthesis and Applications

Abstract

Methods for the preparation of various fused pyrazolothiazoles were reviewed here for the first time. The main types of fused pyrazolothiazole are pyrazolo[5,1-b]thiazoles, pyrazolo[3,4-d]thiazoles, and pyrazolo[4,3-d]thiazoles. Some research and industrial application of pyrazolothiazoles are reported.     

Design,synthesis, and in vitro anticancer screening of novel pyrazolinyl-pyrazole/1, 2, 3-triazole hybrids

Novel hybrids, pyrazolinylpyrazoles, and pyrazolinyltriazoles were designed, synthesized, and screened for their anticancer activity. Eleven compounds were selected by the National Cancer Institute (NCI)/USA for anticancer screening at single high dose (10⁻⁵ M) in full NCI 60 cell panels. Two compounds: 4-aminopyrazole-5-carbonitrile, 5c (NSC-747630/1) and ethyl 4-aminopyrazole-5- carboxylate, 7d (NSC-747634/1) were the most active candidates of the series and were selected for further evaluation at five dose screening as they displayed significant growth inhibition with full panel median growth inhibition (GI₅₀) 5.47 and 2.24 μM, respectively. Both 5c and 7d hybrids exhibited broad spectrum antitumor activity; however 7d showed moderate selectivity (selectivity ratio 3.6) toward leukemia.     

Synthesis,characterization and cytotoxic activity of ferrocenyl hydrazone complexes containing a furan moiety

A ferrocenyl ligand 1 was prepared from condensation of 5-methyl-2-furaldehyde with l,l′-diacetylferrocene dihydrazone. This ligand forms 1:1 complexes with cobalt(II), nickel(II), copper(II) and zinc(II) 2–5 in good yield. Characterization of the ligand and complexes was carried out using infrared, nuclear magnetic resonance, mass spectra, electronic absorption, magnetic susceptibility, molar conductivity, and elemental analysis. Cytotoxic activity of the prepared ligand and its complexes were tested against different human cancer cell lines. The results suggested that the synthesized compounds were more potent than the comparative standards drugs used in most cases, whereas they had less activity in the others.     

Optimal timing decisions for the introduction of new technologies

High technology industries, such as the communications industry, are characterized by frequent development of new technologies. These new technologies are often available before the capacities of existing facilities that use an old technology are exhausted. Whenever a new technology facility is introduced, a fixed set-up cost is generally incurred; however, the annual operating costs are often reduced. The optimal timing of the introduction of new facilities is therefore of interest.In this paper, we examine such timing decisions. The study was motivated by an application involving electronic plug-in units that enhance the operation of communication facilities. First, we develop optimal timing decisions for linearly growing demand. The analysis is then extended to nonlinear demand. For linear demand, one of two decisions is optimal: Either introduce the new technology immediately, or as late as possible. However, for nonlinear demand, these decisions may be nonoptimal.     

A convenient route to pyridones,pyrazolo[2,3‐a]pyrimidines and pyrazolo[5,1‐c]triazines incorporating antipyrine moiety

Condensation of 4‐aminoantipyrine with ethyl acetoacetate, ethyl benzoylacetate, and ethyl cyanoacetate furnished the corresponding ethyl 3‐(1,2‐dihydro‐1,5‐dimethyl‐2‐phenyl‐3‐oxo‐3H‐pyrazol‐4‐yl)aminoacrylate and 2‐cyano‐N‐[(1,2‐dihydro‐1,5‐dimethyl‐2‐phenyl‐3‐oxo‐3H‐pyrazol‐4‐yl)]acetamide derivatives. The aminoacrylates derivatives react with acetonitrile and sodium hydride to give 2‐amino‐6‐methyl‐1‐(1,2‐dihydro‐1,5‐dimethyl‐2‐phenyl‐3‐oxo‐3H‐pyrazol‐4‐yl)‐4‐pyridone. Reaction of the cyanoacetamide derivative with dimethylformamide‐dimethylacetal (DMF‐DMA) afforded 2‐cyano‐N‐[1,2‐dihydro‐1,5‐dimethyl‐2‐phenyl‐3‐oxo‐pyrazol‐4‐yl]‐2‐(N,N‐dimethylamino)methylene acetamide in high yield. Treatment of the latter with 5‐aminopyrazole derivatives afforded the corresponding pyrazolo[2,3‐a]pyrimidines. 2‐cyano‐N‐[(1,2‐dihydro‐1,5‐dimethyl‐2‐phenyl‐3‐oxo‐3H‐pyrazol‐4‐yl)]acetamide also reacts with heterocyclic diazonium salts to give the corresponding pyrazolo[5,1‐c]‐1,2,4‐triazine derivatives. © 2004 Wiley Periodicals, Inc. Heteroatom Chem 15:508–514, 2004; Published online in Wiley InterScience (www.interscience.wiley.com). DOI 10.1002/hc.20046