Synthesis of 1H-pyrazolo[3,4-e]-s-triazolo[3,4-c]-as-triazines, 8H-pyrazolo[3,4-e]tetrazolo[5,1-c]-as-triazine and 1,7-dihydro-8H-pyrazolo[3,4-e]-as-triazine derivatives

3-Hydrazino-7-methyl-5-phenyl-5H-pyrazolo[3,4-c]-as-triazine 1 underwent ring closure and/or condensation reaction with formic acid, acetic acid, acetic anhydride and benzoyl chloride to afford 1H-pyrazolo-[3,4-d]-s-triazolo[3,4-c]-as-triazines 2, 5 and 7a and/or N-acyl derivatives 3, 4 and 6 . N-Acyl derivatives 3 and 6 underwent cyclisation reaction on treatment with phosphoryl chloride to give 5 and 7a . 3-Methyl-1-phenyl-8-aryl-1H-pyrazolo[3,4-e]-s-triazolo[34,-c]-as-triazines 7 were also prepared by the reaction of the hydrazono derivatives 8 wit thionyl chloride. On treatment of 1 with nitrous acid gave the 8H-pyrazolo[3,4-e]tetrazolo-[5,1-c]-as-triazine 9 . Compound 1 underwent ring closure with carbon disulphide or ethyl chloroformate to 1,7-dihydro-8H-pyrazolo[3,4-e]-s-triazolo[3,4-c]-as-triazine derivatives 10 and 12 . Reaction of 1 with ethyl acetoacetate or acetylacetone gave 3-pyrazolo derivatives 13 and 14 .     

SOME REACTIONS OF 3-AMINO-2-CARBOETHOXY-4,6-DIMETHYLTHIENO[2,3-b]-PYRIDINE. SYNTHESIS OF SOME NEW THIENOPYRIDOPYRIMIDINES

Abstract

Thienopyridine oxazinone (1) has been prepared and explored as a precursor by its reaction with some reagents namely, ammonium acetate, aliphatic amines, aromatic amines, hydrazine hydrate, thiosemicarbazide, and ethyl glycinate to give pyridothienopyrimidines (11-VII). The pyrimidinone compound (11) was converted to the 4-chloro derivative (X) by its reaction with excess POCl₃ Interaction of the 4-chlorocompound (X) with some reagents namely, hydrazine hydrate, methyl amine, aniline, sodium thiophenolate, ethyl glycinate, thiosemicarbazide and thiourea, yielded pyridothieno-pyrimidine derivatives (XI-XVII) substituted at 4-position, respectively.     

Validation of scanning electron microscope (SEM), energy dispersive X-ray (EDX) and gamma spectrometry to verify source nuclear material for safeguards purposes

Ten ore samples, two unpurified yellow cake samples and natural uranyl nitrate hexahydrate sample were analyzed by Scanning Electron Microscope (SEM) and Energy Dispersive X-ray (EDX) method to verify source nuclear material. Samples represent source nuclear material as possible. All samples were scanned at ideal conditions; working distance = 10 mm, voltage = 30 kV, magnification value = × 100, spot size = 50 to screen samples for the presence of uranium and thorium, Also Hyper pure germanium (HPGe) gamma spectrometers were applied to estimate the uranium and thorium contents in Bq/kg (ppm). For the ore samples uranium-238 ranges from 1,049.23 Bq/kg (85.30 ppm) to 2,096.06 Bq/kg (170.41 ppm), uranium-235 ranges from 47.51 to 105.61 Bq/kg and thorium-232 ranges from 22.84 Bq/kg (5.65 ppm) to 41.78 Bq/kg (10.34 ppm). For the yellow cake samples and uranyl nitrate hexahydrate uranium-238 ranges from 42.99 Bq/kg (3.50 ppm) to 71,887.2 Bq/kg (5,844.49 ppm) and thorium-232 is 4.78 Bq/kg (1.83 ppm) and the other two samples are lower than the detection limit.     

Facile synthesis and antimicrobial evaluations of some novel pyrazolo[3,4-b]selenolo[3,2-e]pyrazines and their related heterocycles

A new series of pyrazolopyrazinoselenolotriazolopyrimidines was synthesized by a facile method based on condensation of 5-amino-3-methyl-1-phenyl-1H-pyrazolo[3,4-b]selenolo[3,2-e]pyrazine-6-carbonitrile ( 3 ) with triethyl orthoformate followed by intramolecular cyclization with hydrazine to afford 7-amino-8-imino-3-methyl-1-phenyl-1,8-dihydro-7H-pyrazolo[3″,4″:5′,6′]pyrazino[2′,3′:4,5] selenolo[3,2-d]pyrimidine ( 5 ). The latter compound was utilized as a multipurpose precursor for the construction of other new triazoles fused to the pyrazolopyrazino- selenolopyrimidine moiety. Alternatively, acetylation and chloro-acetylation of compound 3 using acetic anhydride and chloroacetyl chloride yielded the acetyl amino 11 and chloroacetamido 12 derivatives, respectively. Compound 12 underwent nucleophilic substitution upon reaction with morpholine to provide the morpholinyl acetamide 13 . Furthermore, the pyrazolopyridoselenolopyrazine ring system 14 was synthesized by the reaction of the o-amino-carbonitrile 3 with malononitrile. Assignment of the chemical structures for the new compounds was confirmed depending on elemental and spectral techniques. On the other hand, most of the synthesized compounds revealed promising results against various bacterial and fungal strains.     

Intransitive Permutation Group with Bounded Movement

Let G be a intransitive permutation group on a set with no fixed point in ; let m, n be a positive integer and let |^g – | m, for every and g G. When G has t orbits and degree n close to [2mp/(p – 1)] + t – 1, this paper constructs such a group with m close to [n(p – 1)/2p].AMS Subject Classification: 20BXX.     

Coupled fixed point theorems for contractions in fuzzy metric spaces

In the present work, we prove a coupled fixed point theorem for contractive mappings in complete fuzzy metric spaces.     

Preparation and Reactions of 2‐Methyl‐7‐(3‐methyl‐5‐oxo‐1‐phenyl‐2‐pyrazolin‐4‐yl)‐5‐arylthiazolo[3,2‐a]‐pyrimido[4,5‐d]oxazin‐4(5H)‐one

Ethyl 7‐amino‐3‐(3‐methyl‐5‐oxo‐1‐phenyl‐2‐pyrazolin‐4‐yl)‐5‐aryl‐5H‐thiazolo[3,2‐a]pyrimidine‐6‐carboxylate was hydrolyzed with an ethanolic sodium hydroxide and the sodium salt thus formed underwent cyclization with acetic anhydride to afford 2‐methyl‐7‐(3‐methyl‐5‐oxo‐1‐phenyl‐2‐pyrazolin‐4‐yl)‐5‐arylthiazolo[3,2‐a]pyrimido[4,5‐d]oxazin‐4(5H)‐one. This compound was transformed to related heterocyclic systems via its reaction with various reagents. The biological activity of the prepared compounds was tested against Gram positive and Gram negative bacteria as well as yeast‐like and filamentous fungi. They revealed in some cases excellent biocidal properties.     

Singular spectrum analysis and Fisher–Shannon analysis of spring flow time series: An application to Anjar Spring,Lebanon

In this study, the time dynamics of water flow from Anjar Spring was investigated, which is one of the major issuing springs in the central part of Lebanon. Likewise, many water sources in Lebanon, this spring has no continuous records for the discharge, and this would prevent the application of standard time series analysis tools. Furthermore, the highly nonstationary character of the series implies that suited methodologies can be employed to get insight into its dynamical features. Therefore, the Singular Spectrum Analysis (SSA) and Fisher–Shannon (FS) method, which are useful methods to disclose dynamical features in noisy nonstationary time series with gaps, are jointly applied to analyze the Anjar Spring water flow series. The SSA revealed that the series can be considered as the superposition of meteo-climatic periodic components, low-frequency trend and noise-like high-frequency fluctuations. The FS method allowed to extract and to identify among all the SSA reconstructed components the long-term trend of the series. The long-term trend is characterized by higher Fisher Information Measure (FIM) and lower Shannon entropy, and thus, represents the main informative component of the whole series. Generally water discharge time series presents very complex time structure, therefore the joint application of the SSA and the FS method would be very useful in disclosing the main informative part of such kind of data series in the view of existing climatic variability and/or anthropogenic challenges.     

Reactions of 4-(2-aminothiazole-4-yl)-3-methyl-5-oxo-1-phenyl-2-pyrazoline. Synthesis of thiazolo[3,2- a ]pyrimidine and imidazo[2,1- b ]thiazole derivatives

4-(2-Aminothiazol-4-yl)-3-methyl-5-oxo-1-phenyl-2-pyrazoline was synthesized via the reaction of 4-bromoacetyl-3-methyl-5-oxo-1-phenyl-2-pyrazoline with thiourea [7] and was transformed to related fused heterocyclic systems. The antifungal and antibacterial studies revealed in some cases excellent biocidal properties.