bluuebunny/crossref_metadata_2025_split huggingface dataset:
An Elegant Synthetic Route to 3-Cyano-5,6-dihydro-2-ethoxy-4-phenyl-pyrido[2,3-a]carbazoles
Authors: Danish Isravel A. , Prasad Karnam J. R. 
Published: August 2018

Abstract
2-Benzylidene-1-oxo-1,2,3,4-tetrahydrocarbazoles (1a - e) obtained from the corresponding 1- oxo-1,2,3,4-tetrahydrocarbazoles on reaction with malononitrile in dry benzene with sodium hydride afforded 3-cyano-5,6-dihydro-2-ethoxy-4-phenyl-pyrido[2,3-a]carbazoles (2a - e) in good yields. A plausible mechanism for the formation of the title compound has been proposed and all the compounds were characterised by IR, NMR, mass spectral methods and elemental analysis.
C-Branched Glycals as Monosaccharidic Push-Pull Butadienes
Authors: Rudloff Ivo , Bari Ahmed , Feist Holger , Michalik Manfred , Reinke Helmut , Peseke Klaus 
Published: August 2018

Abstract
Treatment of 2(3)-formyl-glycals 1, 3, 5 with alkyl cyanoacetates afforded 2(3)-[(E)-2-cyano-2- alkoxycarbonyl-vinyl]-2(3)-deoxy-1,5(2, 6)-anhydro-hex-1(2)-enitols 2, 4, 6 which were reacted with aniline to yield nicotinonitrile acyclo-C-nucleosides 7, 9. Nicotinic acid ester acylo-C-nucleosides 11 were obtained by the reaction of 2,6-anhydro-1,4,5-tri-O-benzyl-3-[(E)-2-cyano-2-alkoxycarbonylvinyl]- 3-deoxy-D-erythro-hex-2-enitols 6 with ammonia.
Preparation and Characterisation of N,N-Disubstituted 2-Amino-5H-selenophenes
Authors: Zug Ines , Hartmann Horst 
Published: August 2018

Abstract
The reaction of N,N’-persubstituted selenoacrylamides with alkyl bromoacetates gives rise to the formation of alkyl derivatives of N,N-disubstituted 2-aminoselenophene-5-carboxylates which can be transformed by saponification into corresponding 5-carboxylic acids. These compounds decompose by heating under formation of hitherto unknown N,N-disubstituted 2-amino-5H-selenophenes their spectral and chemical properties were outlined.
Isoxazolinium Salts in Asymmetric Synthesis. 1. Stereoselective Reduction Induced by a 3’-Alkoxy Stereocentre. A New Approach to Polyfunctionalized β-Amino Acids* [1, 2]
Authors: Henneböhle Marco , Le Roy Pierre-Yves , Hein Matthias , Ehrler Rudolf , Jäger Volker 
Published: August 2018

Abstract
A new approach to optically active N-methylamino acids is presented, relying on stereoselective reduction of N-methylisoxazolinium salts with a dioxyethyl side-chain. The diastereoselectivity of the reduction step is studied systematically, in comparison with that of respective isoxazolines. A two-step transformation of isoxazolinium salts - with NaBH3(OAc) and subsequent catalytic hydrogenation as well as a one-pot reduction by catalytic hydrogenation led to high (95:5 and 87:13) diastereomeric ratios of protected erythro-N-methylaminopentanetriols. The hydroxyethyl side-chain is elaborated by oxidation to afford the β -N-methylamino acid 37, exemplifying the potential of this strategy.
Facile Synthesis of Novel N-Aryl-4,5,6,7-tetrahydro-benzosultams by Oxyfunctionalisation of Bicyclic Isothiazolium Salts*
Authors: Siegemund Anja , Hartung Christine , Eilfeld Alexander , Sieler Joachim , Schulze Bärbel 
Published: August 2018

Abstract
3-Hydroxy- (17a - j) and 3-alkoxy-4,5,6,7-tetrahydro-benzosultams 18a-m were prepared in good yields by oxidation of the bicyclic isothiazolium salts 10 with magnesium monoperoxyphthalate (MMPP·6H2O) in acetonitrile or corresponding alcohol. A HPLC-API-MS(MS) method was used to monitor the oxidation process of 10 with MMPP. 3-Oxo-4,5,6,7-tetrahydro-benzosultams 19a - c, h, j were also obtained.
Neue Barium-Oxoantimonate(III): Darstellung und Kristallstruktur von Ba3[SbO3]2 und Ba2[Sb2O5]/New Barium Oxoantimonates(III): Synthesis and Crystal Structures of Ba3[SbO3]2 and Ba2[Sb2O5]
Authors: Emmerling Franziska , Zimper Sabine , Röhr Caroline 
Published: August 2018

Abstract
The barium oxoantimonates(III) Ba3[SbO3]2 (triclinic, P1̄, a = 615.2(8), b = 981.4(3), c = 1215.4(5) pm, α =74.683(9), β =89.710(6), γ =71.464(7)°, Z =2, R1=0.0802) and Ba2[Sb2O5] (orthorhombic, Cmcm, a = 401.0(3), b = 1450.6(7), c = 636.6(6) pm, Z = 4, R1 = 0.0589) have been synthesized from melts of elemental barium and antimony oxide Sb2O3 at a temperature of 800 °C. Their oxoantimonate building units are strongly influenced by the stereochemically active lone pair electrons of the pentele element: In the Ba rich compound Ba3[SbO3]2, isolated ψ tetrahedra [SbO3]3− are present, in Ba2[Sb2O5], which crystallizes with the Sr2Bi2O5 structure type, two of these ψ tetrahedra are condensed to form nucelar units [Sb2O5]4−. The two compounds are compared in terms of structure and bonding with the alkali antimonates on one hand and with the alkaline earth bismutates on the other.
Magnetic Films of Cobalt/Aluminum Electrodeposited from the Room Temperature Molten Salts AlCl3-BPC-CoCl2
Authors: Yang Chao-Chen , Wu Te-Ho , Shu Min-Fong 
Published: August 2018

Abstract
The electric conductivities of molten mixtures of aluminum chloride-butylpyridinium chloridecobalt chloride (AlCl3-BPC-CoCl2) were measured using a computerized direct-current method. The conductivities of all the melts increased with increasing temperature. The electrodeposition of Co/Al films from the AlCl3-BPC melt containing a small amount of CoCl2 has been studied by cyclic voltammetry. Compact and smooth Co/Al thin films could be obtained at a deposition potential of −0.4 V. The surface morphology and the composition of the electrodeposited thin films were studied using scanning electron microscopy (SEM) and atomic force microscopy (AFM). The magnetic properties of the deposited thin films have been investigated via magnetic force microscopy (MFM) and vibrating sample magnetometry (VSM). Higher magnetization and smooth domains of Co/Al layers could be obtained at the deposition potentials of −0.1 V and −0.4 V, respectively.
Divalent Europium in 1
∞[Eu(Pz)2(Pz-H)2]: The First Unsubstituted Pyrazolate and Cp Analogous Pyrazole Complex of a Rare Earth Element in One
Authors: Quitmann Catharina C. , Müller-Buschbaum Klaus 
Published: August 2018

Abstract
Bright yellow crystals of 1
∞[Eu(Pz)2(Pz-H)2] were obtained by the reaction of europium metal with a melt of pyrazole. According to single crystal X-ray analysis the compound exhibits a onedimensional chain structure including both unsubstituted pyrazolate anions as well as unsubstituted neutral pyrazole molecules as ligands. The latter are isoelectronic with the cyclopentadienyl anion and link two adjacent Europium(II) centers in an η1-σ -bridging as well as Cp analogous η5-π-binding mode, whilst the pyrazolate anions are N-η1-coordinating terminal ligands. In addition to the crystal structure, MIR, FarIR, Raman and UV/vis spectroscopic data are presented.
Convenient Route to Efavirenz Analogues as Potential non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors
Authors: Hamed Atef A. 
Published: August 2018

Abstract
Treating 2-chloro-4-(4-chlorophenyl)-6-methylbenzo[d]-3,1-oxazinium hexachloroantimonate (1) with one equivalent of alcohol or mercaptane led, after hydrolysis with aq. NaOH, to the formation of 4,4-disubstituted-1,4-dihydro-2H-6-methyl-3,1-benzoxazin-2-ones (3). Large excess addition of alcohol afforded either 4’-chloro-2-isocyanato-5-methylbenzophenone disubstitutedketal (4) or N-{2- [(4-chlorophenyl)dialkoxymethyl]-4-methylphenyl} alkylcarbamate (5). Reaction of 4 with primary amines furnished 1-{2-[(4-chlorophenyl)dialkoxymethyl]-4-methylphenyl}-3-substituted urea (6).
The Structure of the Ligand Tri(1-cyclohepta-2,4,6-trienyl)phosphane, P(C7H7)3, in the Hexafluoroacetylacetonato Copper(I) Complexes, (hfac)Cu[P(C7H7)3]n (n = 1, 2)
Authors: Herberhold Max , Milius Wolfgang , Akkus Nilgün 
Published: August 2018

Abstract
The reaction of CuCl[P(C7H7)3] (1a) with sodium hexafluoroacetylacetonate, Na(hfac), leads to (hfac)Cu[P(C7H7)3] (2a), which in the presence of excess P(C7H7)3 (a) gives (hfac)Cu[P(C7H7)3]2 (3a). Whereas the 1:2 compound 3a is a pseudo-tetrahedral copper(I) complex with relatively long Cu-P (224.85(10) and 223.75(10) pm) and Cu-O (212.7(3) and 212.0(3) pm) distances, the 1:1 complex 2a may be described as having a distorted pseudo-trigonal coordination sphere (Cu-P 214.32(11) pm, Cu-O 196.6(3) and 208.1(3) pm), although one of the cyclohepta-2,4,6-trienyl substituents develops a weak additional interaction with the metal through its central C=C double bond (Cu-C 275.1 and 272.9 pm). The molecular geometries of the tri(1-cyclohepta-2,4,6-trienyl) complexes 2a and 3a are compared with those of the known tri(cyclohexyl)phosphane complexes, (hfac)Cu[P(C6H11)3]n (n = 1 (2b) and 2 (3b)), and related compounds.
Optically Active Transition Metal Compounds, 136 [1]. An Octahedral Molybdenum Complex (P-P’)Mo(CO)4 with a Chiral Secondary Phosphorus Atom
Authors: Brunner Henri , Grau Ilias , Zabel Manfred 
Published: August 2018

Abstract
Reaction of (η6-C6H5CH3)Mo(CO)3 with the easily accessible chiral chelate ligand P,P,Pʹ-tris- [(+)-9-phenyldeltacyclan-8-yl]-1,2-bis(phosphanyl)benzene P-P’ afforded the octahedral molybdenum carbonyl derivate (P-P’)Mo(CO)4 1 as a diastereomer mixture 1a (74%) and 1b (26%). Crystallization gave single crystals of (SP)-(P-P’)Mo(CO)4 1a. The X-ray structure analysis of compound 1a revealed the formation of an unusual triple-decker π-stack in the solid state.
Synthesis and Biological Evaluation of a “Natural” Insect Repellent
Authors: Csuk René , Niesen Anja 
Published: August 2018

Abstract
(11Z)-11,19-Icosadienyl acetate (1) has been shown to be an efficient repellent against the ant Myrmica rubra whereas its corresponding (11E) stereoisomer 2 does not exhibit any repellent activity at all. Several synthetic strategies for these two compounds have been evaluated.
Homoleptic Nickel(0) Phenyl Isocyanide Complexes
Authors: Hahn F. Ekkehardt , Münder Marco , Fröhlich Roland 
Published: August 2018

Abstract
The tetrakis(phenyl isocyanide)nickel(0) complexes [Ni(CNR)4](R = C6H5, 1; R= C6H3-2,6-Me2, 2; R = C6H4-2-NO2, 3) have been synthesized from [Ni(COD)2] and the corresponding phenyl isocyanides in toluene. Complexes 1 - 3 were characterized by X-ray diffraction. All three complexes contain a nickel atom which is coordinated in a slightly distorted tetrahedral fashion.
Chirale Erkennung bei Tris(diimin)-Metallkomplexen, 10. Vergleich der intermolekularen Wechselwirkungs- und Packungsmuster in der Reihe [Cr(bpy)3]n+(PF6)n (n = 0 – 3) / Chiral Recognition among Tris(diimine)-metal Complexes, 10. Comparison of Intermolecular Interactions and Packing Patterns in the Series [Cr(bpy)3]n+(PF6)n (n = 0–3)
Authors: Breu Josef , Zwicknagel Andrea 
Published: August 2018

Due to their conformational rigidity, the corrugated, chiral molecular structure, and the variability in the central metal and its oxidation state, [M(bpy)3]n+ complexes are particularly well suited to study chiral recognition and to identify intermolecular interaction patterns in the crystalline state. For [Cr(bpy)3]n+(PF6)n (n=0 - 3) four oxidation states are readily accessible which allows to investigate the influence of the cation/anion ratio on the observed packing patterns.
The crystal structures of all four oxidation states are governed by so-called ‘π-π-interactions’. Apparently, in molecular salts the Madelung energy is less important as compared to classical inorganic salts.
Interestingly, [Cr(bpy)3](PF6) and [Cr(bpy)3](PF6)2 comprise the same homochiral layers. However, while the former crystallises as true racemate, the latter spontaneously resolves into a conglomerate. This two-dimensional building block of homochiral layers is the most popular structural motif in this class of compounds which has been observed in a great variety of racemic and homochiral stackings.
Crystal Engineering of a New Layered Polyiodide Using 1,9-Diammoniononane as a Flexible Template Cation
Authors: Reiß Guido J. , Engel Judith S. 
Published: August 2018

Abstract
The reaction of 1,9-diaminononane with hydroiodic acid in the presence of iodine gave a compound best described as 1,9-diammoniononane bis-triiodide iodine, (H3N-(CH2)9-NH3)[I3]2 · I2. The structure is built from two crystallographically independent I3
− anions, which are connected via secondary I···I interactions to the iodine molecules, and the 1,9-diammonioalkane cations are connected via weak hydrogen bonds to neighbouring iodine atoms. By a cooperative phenomenon, the shape and the functionality of the cation lead to a solid state structure that includes a polyiodide substructure with the formula 2
∞[I8]2− or 2
∞[I3 · I2 · I3]2−, is best described as a brick-shaped layered array. Its rectangular pores fit excellently with the hydrogen bonding functionality as well as with the conformational needs of the 1,9-diammoniononane template. The Raman spectrum shows typical bands of coordinated triiodide anions and iodine molecules. The thermal analysis (DSC/TG) of the title compound indicates decomposition at temperatures above 210°C.
Synthesis and Solid-State Structures of Alkyl-Substituted 3-Cyano-2-pyridones
Authors: Fischer Christian B. , Polborn Kurt , Steininger Harald , Zipse Hendrik 
Published: August 2018

Abstract
A series of 3-cyano-pyridones carrying a variety of alkyl substituents at C-5 and C-6 has been synthesized and their solid-state structures have been studied. Hydrogen bonding interactions between individual pyridone molecules lead either to the formation of symmetric dimers of the R2
2 (8) type or to helical chains of the C(4) type. Based on known and calculated structures for the 2-pyridone parent system, the solid-state structures can be divided in two groups representing cases with little external influence on the hydrogen bonding array (group A) and those with a larger external influence (group B).
Synthesis, Spectroscopic Studies and Crystal Structure of 5,5’-Dimethoxy- 3,3’-methanediyl-bis-indole as the Inhibitor of Cell Proliferation of Human Tumors
Authors: Maciejewska Dorota , Niemyjska Maria , Wolska Irena , Włostowski Marek , Rasztawicka Magdalena 
Published: August 2018

Abstract
5,5’-Dimethoxy-3,3’-methanediyl-bis-indole (3) was synthesized in a reductive cyclisation process from (E)-5-methoxy-2-nitro-β -morpholinestyrene. The solid state structure was probed by single crystal X-ray diffraction and 13C CP/MAS NMR methods. The results of the X-ray analysis indicate insignificantly different structure of both methoxyindole fragments of the molecule, and this is the main reason for the appearance of the double resonances in the solid state NMR spectrum. Interesting N-H· · ·π interactions were observed which may have a functional role in biological features of 3. 5,5’- Dimethoxy-3,3’-methanediyl-bis-indole at conc. 1 · 10−4 M reduces the growth of MCF7 (breast), NCI-H460 (lung), and SF-268 (NCS) cells to 21, 0, and 48%, respectively.
Luminescent Gold(I)-Thallium(I) Arrays through N-Bidentate Building Blocks
Authors: Fernández Eduardo J. , Jones Peter G. , Laguna Antonio , López-de-Luzuriaga José M. , Monge Miguel , Montiel Manuel , Olmos M. Elena , Pérez Javier 
Published: August 2018

Abstract
Heteropolynuclear gold(I)-thallium(I) complexes of the type [TlLn][Au(C6F5)2] (L = py (2), 2,2’- bipy (3), 1,10-phen (4) or 4,4’-bipy and THF (5); n = 1, 2) have been obtained from reactions of the corresponding N-donor ligands with the precursor {Tl[Au(C6F5)2]}n (1). The crystal structures of complexes 3 - 5 have been determined by X-ray diffraction showing one- (3, 4) or three-dimensional (5) arrays. All complexes are photoluminescent in the solid state at RT and at 77 K. The strong visible emissions of complexes 2 - 5 are displayed over a wide range of wavelengths (460 - 620 nm) depending on the environment of the thallium(I) centres and on the nature of the N-donor ligand.
Crystal and Molecular Structure of P(C6H5)5 · 0.5 THF
Authors: Müller Gerhard , Bildmann Ulrich Jürgen 
Published: August 2018

Abstract
Pentaphenylphosphorus crystallizes from tetrahydrofuran (THF) as P(C6H5)5・0.5 THF (triclinic space group: P1̅, a = 10.095(4), b = 10.252(3), c = 12.725(3) A° , α = 71.21(1), β = 76.98(3), γ = 87.12(1)°, Z = 2). Its molecular structure is an almost perfect trigonal bipyramid with significantly longer axial than equatorial P-CPh bonds (P-Cax 1.982(2)/1.979(2), P-Ceq 1.853(2)/1.845(2)/1.847(2) Å). It differs from the well established structure of solvent-free P(C6H5)5 (P. J. Wheatley, J. Chem. Soc. 2206 (1964)) in the relative orientation of the phenyl rings with respect to each other (axial rings) and with respect to the equatorial PC3 plane (equatorial rings) but not in the trigonal-bipyramidal (tbp) geometry at phosphorus. Differences in the geometry around the central atom had been found previously for Sb(C6H5)5 (square pyramid) and Sb(C6H5)5 · 0.5C6H12 (tbp) but not in As(C6H5)5 and As(C6H5)5 · 0.5 C6H12 (both tbp).
Intramolecular Carbene and Carbenoid Reactions of α-(Vinyloxy)silyl-α-diazoacetates
Authors: Daucher Birgit , Gettwert Volker , Striegler Ruth , Maas Gerhard 
Published: August 2018

Abstract
Thermolysis of α-[diisopropyl-1-(methylvinyl)oxysilyl]-α-diazoacetate 5a at 160 °C yields mainly 2,5-dihydro-1,2-oxasilole-3-carboxylate 6a and 3-[diisopropyl(methoxy)silyl]-2(5H)-furan- 2-one 7. From the thermolysis reaction of α-[diisopropyl-1-(phenylvinyl)oxysilyl]-α-diazoacetate 5b, only 1-oxa-2-sila-3-cylopentene-3-carboxylate 6b could be isolated in low yield. UV-irradiation of 5a,b generates 6a,b as the main products. The Rh2(C3F7COO)4-catalyzed decomposition of 5a provides primarily the ketene 2-[diisopropyl(methoxy)silyl]-pent-1-ene-1,4-dione (9) in high yield. After work-up, 3-[diisopropyl(methoxy)silyl]-2(3H)-furan-2-one 10a and 2(5H)-furanone 7 are obtained in relative amounts that depend on work-up conditions. Mechanistic pathways leading to the various products are proposed.
Introduction of Perfluoroalkyl Substituents into Heteroarenes via Nucleophilic Substitution of Hydrogen
Authors: Mąkosza Mieczysław , Loska Rafał 
Published: August 2018

Abstract
A summary of research in the area of fluoroalkylation of electron-deficient aromatic compounds is presented. The reaction of dinitro- and cyanonitroarenes with trifluoromethyl-trimethylsilane (Me3SiCF3) and tris(dimethylamino)sulfonium difluorotrimethylsilicate (TASF) and subsequently with DMD provides trifluoromethylated cyano- and nitrophenols via oxidative nucleophilic substitution of hydrogen. Addition of fluorinated carbanions, generated either by addition of F− anions to hexafluoropropene or by activation of Me3SiCF3, to N-alkylazinium salts leads to dihydropyridines, dihydroquinolines etc., oxidation of which affords the respective fluoroalkylated heterocycles.
1,3-Dipolar cycloaddition of azine N-oxides to hexafluoropropene gives 2-heteroaryl-2,3,3,3-tetrafluoropropionic acid fluorides, which react with various protic nucleophiles to give esters and amides of 2-heteroarylperfluoropropionic acids, whereas reaction with water and decarboxylation of the free acids gives azines with a 1,2,2,2-tetrafluoroethyl group at C-2.
Thia- and Selena-Heterocycles Containing Cycloamidine Substructures: Ring Contraction Reactions of 1,3,4-Thia-/Selenadiazines
Authors: Fleischhauer Jan , Beckert Rainer , Hornig David , Günther Wolfgang , Görls Helmar , Klimesova Vera 
Published: August 2018

Abstract
1,3,4-Thia/selena-diazines proved to be suitable starting materials for ring contraction reactions. Treatment with acetic acid/water mixtures leads to highly substituted 1,3,4-thia/selenadiazoles. In addition, the selenadiazoles formed undergo a fast Dimroth-rearrangement to finally yield derivatives of 1,2,4-triazole. The structures of all new derivatives were confirmed by NMR experiments, mass spectroscopy, elemental analysis and X-ray structural analysis.
New Approaches to Branched β-Amino α-Hydroxy Acids, Taxol Side-chain Analogs
Authors: Li Feng , Li Zhao-Ming , Yang Hua , Jäger Volker 
Published: August 2018

Abstract
The phenylisothreonine derivatives, taxol side-chain analogs, were synthesized by two routes, one based on the highly stereoselective addition of a phenyl Grignard reagent to the L-threose-derived nitrone 7, and the other using asymmetric α-alkoxyallylation of the ketimine 20 with chiral allyl boron reagents.
Structural Characterization of Cationic 16-Electron Pentamethylcyclopentadienyl Ruthenium(II) Complexes Containing the Binuclear [Cp*Ru(μ-Cl)3RuCp*]– Anion
Authors: Glöge Thomas , Petrovic Dejan , Hrib Cristian G. , Jones Peter G. , Tamm Matthias 
Published: August 2018

Abstract
The reaction of the diimine ligand 1,2-bis(1,3-diisopropyl-4,5-dimethylimidazolin-2-imino)ethane (BLiPr) with tetrameric [Cp*RuCl]4 in a 1 : 0.75 ratio afforded the complex salt [1][2] containing the 16-electron half-sandwich cation [Cp*Ru(BLiPr)]+ (1) and the dinuclear anion [Cp*Ru(μ- Cl)3RuCp*]− (2). The X-ray crystal structures of [1][2]·31/2THF (monoclinic, space group P21/n, Z = 4) and of [1][2]·THF (monoclinic, space group C2/m, Z = 4) are reported, allowing the structural characterization of the unprecedented anion 2, in which two [(η5-C5Me5)Ru(II)] moieties are bridged by three μ2-chlorine atoms.
Diazadioxacyclophanes
Authors: Bartsch Richard A. , Jones Peter G. , Kuś Piotr , Dix Ina 
Published: August 2018

Abstract
Six new cyclophane molecules (5 - 10) were synthesized from α,α´-bis(N-tosyl-4-aminophenyl)- 1,4-diisopropylbenzene and α,α´-bis[4-(n-bromoalkyloxy)phenyl]-1,4-diisopropylbenzene. The crystal and molecular structures of α,α´-bis(4-aminophenyl)-1,4-diisopropylbenzene (3), α,α´-bis (N-tosyl-4-aminophenyl)-1,4-diisopropylbenzene 4 and the ditosyl derivative of the diazadioxacyclophane 6 were determined. The noncyclic compounds 3 and 4 display the anti conformation. Diazadioxacyclophane 6 possesses a central cavity that might be exploited to accommodate guest molecules, but some conformational change would probably be required.
Synthesis and Anticancer Evaluation of Some New 4-Amino-3- (p-methoxybenzyl)-4,5-dihydro-1,2,4-triazole-5-one Derivatives
Authors: Bekircan Olcay , Kucuk Murat , Kahveci Bahittin , Bektas Hakan 
Published: August 2018

Abstract
4-Amino-3-p-methoxybenzyl-5-oxo-4,5-dihydro-1,2,4-triazol-1-yl-acetic acid ethyl ester (2) was prepared from 4-amino-4,5-dihydro-1H-1,2,4-triazole-5-one (1) and ethyl bromoacetate. Compound 3 was synthesized by the condensation of 2 with hydrazine hydrate. The treatment of compound 3 with various aromatic aldehydes resulted in the formation of arylidene hydrazides as cistrans conformers 4a - g. Thiosemicarbazide derivative 5 was prepared by the reaction of compound 3 with phenylisothiocyanate. Cyclization of 5 with sodium hydroxide resulted in the formation of compound 6. Treatment of 6 with benzyl bromide gave compound 7. Four of the newly synthesized compounds were screened for their anticancer activity against a panel of 60 cell lines derived from nine cancer types, namely, non-small cell lung, colon, breast, ovarian, leukemia, renal, melanoma, prostate and CNS cancers at a fixed dose of 10 μM.
A prenylated acridone alkaloid and ferulate xanthone from barks of Citrus medica (Rutaceae)
Authors: Fomani Marie , Happi Emmanuel Ngeufa , Kouam  , Francois-Hugues Poree , Lallemand Marie-Christine , Kamdem Waffo Alain François , Wansi Jean Duplex 
Published: August 2018

Abstract
A new prenylated acridone alkaloid, medicacridone (1), and a new ferulate xanthone, medicaxanthone (5), together with 11 known compounds were isolated from the methanol extract of the bark of the Cameroonian medicinal plant Citrus medica. The structures of all compounds were determined by comprehensive analyses of their 1D and 2D NMR, mass spectral (EI and ESI) data, chemical reactions, and comparison with previously known analogues. The agar diffusion test delivered low to missing antimicrobial activities, corresponding with MICs > 1 mg mL–1, while compounds 1–6 and atalantoflavone (9) displayed weak cytotoxic activity against the human Caucasian prostate adenocarcinoma cell line PC-3, with IC50 values ranging from 60.5 to 80.0 μm
versus doxorubicine with IC50=0.9 μm.