Synthesis of Substituted 4‐Aroyl‐1‐indanone and 5‐Aroyl‐1‐tetralone

Several substituted 4‐aroyl‐1‐indanones 2 and 5‐aroyl‐1‐tetralones 3 were prepared in good yields from 1‐indanones 1 via a series of reasonable transformations.     

A new convenient synthesis of aroyl cyanides via the formation of cyanohydrin nitrate intermediates

The treatment of α-bromoarylacetonitriles with AgNO₃ generates cyanohydrin nitrate intermediates, which easily eliminate nitrous acid with the formation of carbonyl bond to afford aroyl cyanides in good to high yields.     

Mizoroki-Heck type arylation of alkenes using aroyl chlorides under base-free conditions

The Mizoroki-Heck type arylation of alkenes with aroyl chlorides accompanied by decarbonylation efficiently proceeds in the presence of a palladium catalyst system, PdCl₂(PhCN)₂/(PhCH₂)Bu₃NCl, even without adding any base. The products can be isolated by a very simple procedure.     

Microwave-assisted synthesis of new pyrimido[4′,5′:4,5]thiazolo[3,2-a]benzimidazol-4(3H)-one derivatives in solvent-free condition

Microwave-assisted synthesis of new 2-arylpyrimido[4′,5′:4,5]thiazolo[3,2-α]benzimidazol-4(3H)-ones from 3-aminothia- zolo[3,2-α]benzimidazol-2-carboxamide and aroyl halides in solvent-free condition is described.In comparison with classical conditions the reactions are faster and the yields are higher under microwave irradiation.     

Microwave-assisted synthesis of new pyrimido[4′,5′：4,5]thiazolo[3,2-α] benzimidazol-4（3H）-one derivatives in solvent-free condition

Microwave-assisted synthesis of new 2-arylpyrimido[4′,5′：4,5]thiazolo[3,2-α]benzimidazol-4（3H）-ones from 3-aminothia- zolo[3,2-α]benzimidazol-2-earboxamide and aroyl halides in solvent-free condition is described. In comparison with classical conditions the reactions are faster and the yields are higher under microwave irradiation.     

α－芳甲酰基烯酮二硫缩醛的新合成方法

以碳酸钾为碱，芳甲酰丙酮（１）与二硫化碳、卤代烃反应得到２－乙酰基－２－芳甲酰基烯酮硫代缩醛（２），２在乙硫醇钾作用下脱乙酰基生成标题化合物（３）。１→３的转化具有反应条件温和、产物产率高及对３中各种缩醛基均可通用等特点。     

A new organic transformation by introducing crotyl/allyltrifluoroborates in cross-coupling reaction with aroyl chlorides

Microwave irradiated PdCl₂(d^tbpf) catalyzed direct cross-coupling reaction of aroyl chlorides with potassium crotyl/allyltrifluoroborates has been developed. Regioselectivity of the cross-coupling product is varied from crotyltrifluoroborate to allyltrifluoroborate.     

1-芳酰基-4-(1＇-N-β-D-吡喃型糖基)氨基硫脲类化合物的合成

通过2,3,4,6-四-O-乙酰基-β-D-吡喃型葡萄糖异硫氰酸酯和2,3,4-三-O-乙酰基-β-D-吡喃型木糖异硫氰酸酯与取代的芳基酰肼的亲核加成反应合成了10个1-芳酰基-4-(1＇-N-2＇,3＇,4＇,6＇-四-O-乙酰基-β-D-吡喃型葡萄糖基)氨基硫脲和7个1-芳酰基-4-(1＇-N-2＇,3＇,4＇-三-O-乙酰基-β-D-吡喃型木糖基)氨基硫脲,所得化合物的结构经元素分析,IR,1H NMR确证.     

Regioselective oxidative ring-opening of cyclopropenyl carboxylates by visible light photoredox catalysis

Catalyzed by Ir(dFCF₃ppy)₂(dtbbpy)PF₆, several aroyl methylidenemalonates were synthesized in good to excellent yields via visible light photoredox-catalyzed the oxidative ring-opening of cyclopropenyl carboxylate derivatives. The possible mechanism of oxidative quenching cycle was proposed.     

1-芳酰基-4-(1'-N-β-D-吡喃型糖基)氨基硫脲类化合物的合成(英文)

通过 2 ,3,4 ,6 四 O 乙酰基 β D 吡喃型葡萄糖异硫氰酸酯和 2 ,3,4 三 O 乙酰基 β D 吡喃型木糖异硫氰酸酯与取代的芳基酰肼的亲核加成反应合成了 1 0个 1 芳酰基 4 ( 1′ N 2′,3′,4′,6′ 四 O 乙酰基 β D 吡喃型葡萄糖基 )氨基硫脲和 7个 1 芳酰基 4 ( 1′ N 2′,3′,4′ 三 O 乙酰基 β D 吡喃型木糖基 )氨基硫脲 ,所得化合物的结构经元素分析 ,IR ,1 HNMR确证 .     

N-邻甲氧基苯甲酰基-N'-芳酰氨基硫脲的合成与抑菌活性研究

由邻甲氧基苯甲酰氯与硫氰酸钾反应生成邻甲氧基苯甲酰基异硫氰酸酯,再与芳酰肼进行加成反应,合成了8种邻甲氧基苯甲酰基芳酰氨基硫脲衍生物,其结构经元素分析、红外光谱和1H NMR确证.初步的生物活性测试结果表明,该类化合物对枯草杆菌有抑制作用,而对大肠杆菌无明显的抑制作用.     

Reaction of N-methylazomethine ylide with aroyl azides: Synthesis of imidazolidin-4-ones

Aryl isocyanates generated in situ from aroyl azides react with N-methylazomethine ylide generated in situ from N-methylspiroanthraceneoxazolidine at 210?°C in a microwave reactor to form 3-arylimidazolidin-4-ones in 30–81% yield.     

A General Synthesis of Functionalized Primary t-Alkylamines

A simple and efficient γ-acetamidopropylation of different nucleophiles using oxazine 3 has been developed. Deacetylation of acetamides with titanium(IV) isopropoxide/diphenylsilane is also described.     

Synthesis,characterization, and biological activity studies on (E)-N′-[2-hydroxy-1,2-di(pyridin-2-yl)ethylidine]aroyl hydrazides and their copper(II) complexes

The reaction of copper(II) salts with (E)-N-(2-hydroxy-1,2-di(pyridin-2-yl)ethylidene)aroyl hydrazide (H₂L¹, H₂L², H₃L³) or (E)-N-(2-hydroxy-1,2-di(pyridin-2-yl)ethylidene) isonicotinohydrazide (H₂L⁴) afforded the complexes [(L)Cu(H₂O)₃], [(H₂L)Cu(OAc)(H₂O)], [(HL)Cu(OAc)] _n , [(H₂L)Cu(H₂O)](ClO₄)₂ and [(H₂L)Cu(OAc)(H₂O)], where n = 1 or 2 and L is the dinegative ion of the ligands. The ligands and their complexes are characterized by elemental analyses, spectral (IR, NMR, electronic, and ESR) and magnetic studies. The FT-IR indicates that the ligands are neutral or anionic polydentate. The number of the coordinating centers depends on the nature of the metal used and the reaction conditions. The room temperature magnetic moment values, electronic spectra and ESR data indicate square planar, trigonal bipyramidal, square pyramidal, and distorted octahedral ligand fields around copper(II). Thermal decomposition of the complexes was monitored by TG and DTG under N₂ and the thermal decomposition mechanisms are given. The compounds were screened for their antimicrobial activities on some Gram-positive and Gram-negative bacterial species. The free ligands are inactive against all studied bacteria. The complexes have variable activity with the most active [(H₂L)Cu(H₂O)](ClO₄)₂, where H₂L is H₂L¹ or H₂L². The minimum inhibition concentrations for these two complexes were determined. These biological activity results are related to the structures of the compounds.     

Synthesis of dialkyl 5-(aryl)-1-phenyl-1H-prazole-3,4-dicarboxylates via a one-pot and four-component reaction

A number of new dialkyl 5-(aryl)-1-phenyl-1H-prazole-3,4-dicarboxylate derivatives have been prepared regiospecifically in moderate to good yield from the cyclocondensation reaction of dialkyl (E)-2-(dialkoxyphosphoryl)-3-(aroyl)-2-butenedioate, derived from the reaction between trimethyl phosphite, an acetylenic ester, and an aroyl chloride, with phenylhydrazine. The reaction is four-component and is carried out under reflux conditions in dry toluene.     

Synthesis of (3,6-dihydro-2H-pyran-2-yl)phosphonate derivatives and investigation of catalyst effect on frontier molecular orbitals using DFT method

Hetero Diels-Alder (HDA) reactions between 2,3-dimethyl-1,3-butadiene and diethyl ester of aroyl phosphonates catalyzed by AlCl₃ to afford (3,6-dihydro-2H-pyran-2-yl) phosphonate derivatives were investigated. Aroyl phosphonates with electron-withdrawing groups generally resulted in better isolated chemical yields. A stoichiometric amount of AlCl₃ rather than a catalytic amount was necessary to activate the cycloaddition reaction. The amount of AlCl₃ catalyst and its effect on LUMO of ethyl ester benzoyl phosphonate were also investigated by performing density functional theory (DFT) (B97D/6-31+G(d,p)) computations in dichloromethane. An increased loading of AlCl₃ induced a considerable decrease in the LUMO energy of ethyl ester of benzoyl phosphonate. The computed Gibbs free activation energy is 17.03 kcal/mol in DCM at 0°C using the same computational level.     

Multiwalled Carbon Nanotubes Supported Pd(II)‐Salen Complex: An Effective,Phosphorous‐Free,and Reusable Heterogeneous Precatalyst for the Synthesis of Diaryl Ketones

The Suzuki–Miyaura cross‐coupling reaction of aroyl chlorides and arylboronic acids has been carried out efficiently in the presence of Pd(II)‐salen@MWCNTs as an air‐moisture stable precatalyst. The influence of various parameters, such as solvent, temperature, and base on the reaction system, was studied. Furthermore, the catalyst can be easily recovered quantitatively by a simple filtration and reused for three consecutive runs without significant loss of its activity.     

Synthesis and spectroscopic studies of copper(II) and nickel(II) complexes containing hydrazonic ligands and heterocyclic coligand

Two types of copper(II) and nickel(II) complexes derived from benzophenone anthranoylhydrazone (L1), 2-acetonaftanone anthranoylhydrazone (L2), 4-phenylacetonaftonone anthranoylhydrazone (L3), benzophenone salicyoylhydrazone (L4), 2-acetonaftanon salicyoylhydrazone (L5), 4-phenylacetonaftanon salicyoylhydrazone (L6) and bidentate heterocyclic base [1,10-phenanthroline (phen)] with general stoichiometry [ML2] and [ML(phen)]Cl have been synthesized and characterized by elemental analysis, infrared spectra, UV-vis electronic absorption spectra and magnetic susceptibility measurements. The effect of varying pH and solvent on the absorption behavior of both ligands and complexes have been investigated. According to the IR spectra, the ligands act as monobasic bidentate and coordination takes place in the enol tautomeric form.     

Crystal engineering with aroyl hydrazones of diacetyl monooxime – Molecular and supramolecular structures of two Ni(II) and two Zn(II) complexes

Four new Schiff bases of aroyl hydrazides with diacetyl monooxime have been prepared, and Ni(II) and Zn(II) complexes of these ligands have been synthesized. Two Ni(II) and two Zn(II) complexes have been characterized by X-ray crystallography. The aroyl hydrazone ligands were designed in such a way that there is a systematic variation in the H-bond forming abilities of their aroyl moiety, e.g. both H-bond acceptor and donor (salicyloyl), only H-bond donor (anthraniloyl), only H-bond acceptor (isonicotinoyl). It is shown in this work that such a variation in the H-bond donor acceptor properties of the ligands leads to considerable diversity in their supramolecular architecture.