Synthesis of novel pyrazole‐based triazolidin‐3‐one derivatives by using ZnO/ZrO2 as a reusable catalyst under green conditions

An efficient approach for the synthesis of 10 novel pyrazole‐based 1,2,4‐triazolidin‐3‐one derivatives catalyzed by ZnO‐loaded ZrO₂ as heterogeneous catalyst with ethanol as solvent is described. The structure of the mixed metal oxide catalyst was characterized by various instrumental techniques (scanning electron microscopy, transmission electron microscopy, X‐ray diffraction and Brunauer–Emmett–Teller). In smooth reactions, products were accomplished in excellent yields (90–94%) with short reaction times (≈ 45 min). ZnO/ZrO₂ catalyst exhibited good recyclability. The catalyst is reused six times without any noticeable loss of activity. The major advantages of this method are operational simplicity, mild conditions, simple work‐up procedure and broad functional group tolerance.     

Late-Stage Chemoenzymatic Installation of Hydroxy-Bearing Allyl Moiety on the Indole Ring of Tryptophan-Containing Peptides

The late-stage functionalization of indole- and tryptophan-containing compounds with reactive moieties facilitates downstream diversification and leads to changes in their biological properties. Here, the synthesis of two hydroxy-bearing allyl pyrophosphates is described. A chemoenzymatic method is demonstrated which uses a promiscuous indole prenyltransferase enzyme to install a dual reactive hydroxy-bearing allyl moiety directly on the indole ring of tryptophan-containing peptides. This is the first report of late-stage indole modifications with this reactive group.     

Amorphous metal-aluminophosphate catalysts for aldol condensation of n-heptanal and benzaldehyde to jasminaldehyde

Amorphous aluminophosphate (AlP) and metal‐aluminophosphates (MAlPs, where M=2.5 mol%Cu, Zn, Cr, Fe, Ce, or Zr) were prepared by coprecipitation method. Their surface properties and catalytic activity ...     

Trace elements in the scalp hair of patients with alcohol induced psychosis

A number of essential trace elements play a major role in various metabolic pathways and in many diseases like autoimmune, neurological and psychiatric. This study is undertaken with an aim to evaluate the levels of different trace elements in the scalp hair samples of patients suffering from alcohol induced psychosis by particle induced X-ray emission technique (PIXE). It is observed that Fe (p?<?0.0005), Cu (p?<?0.001) are significantly higher in the hair samples of alcohol induced psychosis patients compared to those in normals while concentrations of Mn (p?<?0.005) and Zn (p?<?0.0001) are lower. The concentrations of Co and Ni in the hair samples are found to be in consonance with the concentrations in the normals.     

Synthesis of 4H-chromene-isoxazole hybrids via ortho-hydroxy directing cyclization of isoxazole-styrenes and Michael addition of imino-chromenes in aqueous medium

A green, efficient, and one-pot method synthesis of functionalized 4H-chromene-isoxazole hybrids is reported via o-hydroxy group directing cyclization of isoxazole-styrenes and Michael addition of 3,5-dimethyl-4-nitroisoxazole on 2-imino-2H-chromene-3-carbonitrile (independent methods). The developed methodology was further extended for nitromethane, malononitrile, and alkylcyanoacetates as Michael donors.     

Iodine mediated synthesis of some new imidazo[1,2-a]pyridine derivatives and evaluation of their antimicrobial activity

Herein, we reported a series of new 2-(5-methyl-1-aryl-1H-1,2,3-triazol-4-yl)imidazo[1,2-a]pyridines by using iodine and NH₄OAc in good yields. The structures of the titled compounds were characterized by the elemental analysis, ¹H NMR, ¹³C NMR, IR, and mass spectral analysis. All the titled compounds were screened for their in vitro antibacterial and antifungal activities by using streptomycin and Nystatin as standard drugs. The compounds 3k , 3l , 3g , and 3c exhibited potent activity against the tested bacterial strains and 3k , 3l , and 3c exhibited potent activity against the tested fungal strains than the reference drugs.     

New class of diethyl substituted phosphoramidimidates and phosphonimidates: synthesis,spectral characterization and antimicrobial activity

Abstract

A series of new class of diethyl N-2-hydroxyethyl-N'-substituted phosphoramidimidates 6(a–e) and diethyl P-morpholino-N-substituted phosphonimidates 6(f–j) was synthesized. The precursor intermediates, diethyl substituted phosphoramidites 3(a–b) were prepared initially by a reaction of various amines 1(a–b) and diethyl phosphorochloridite (2) and then they were treated by in situ with aromatic/alkyl azides through Staudinger reaction to accomplish title products. Structures of all the synthesized compounds were characterized by spectroscopic data such as IR, NMR (¹H, 13C, ³¹P), mass, and elemental analyses. The synthesized compounds were screened for their in vitro antimicrobial activity to understand their biological potency. The biological screening results disclosed that compounds 6b, 6c, 6e, 6g, 6h and 6j having potent antimicrobial activity against all the tested pathogens.     

Crystal and molecular structure of 6- t -butyl-3-cyclohexyl-3,4-dihydro-2-(2-chlorophenoxy)-2H-1,3,2-benzoxazaphosphorine-2-oxide

The structure of the title compound was determined by the Patterson method and refined to anR of 0·10 for 8065 observed reflections. The crystals are triclinicP1,a=12·408(2),b=13·157(2),c=14·479(8)?, α=74·706(8), β=88·728(9), γ=88·660(13)° withZ=4. The intensity data were collected on an Enraf-Nonius CAD-4 single crystal X-ray diffractometer. The benzoxazaphosphorine ring adopts a conformation intermediate between a half-chair and a sofa with the phosphoryl oxygen O(2) in an axial and the 2-chlorophenyl andt-butyl groups which aretrans to each other in equatorial positions. The cyclohexyl ring adopts a chair conformation with the nitrogen atomN(5) in an equatorial position. In one conformation of the molecule (I) thet-butyl group atoms and one of the carbon atoms, C(24) in the cyclohexyl ring are disordered. In the other conformation (molecule II) the 2-chlorophenyl ring adopts a conformation midway between a half-chair and a sofa. The molecular packing involves mainly van der Waals contacts.     

Separation and determination of synthetic impurities of sildenafil (Viagra) by reversed-phase high-performance liquid chromatography.

A simple and rapid high-performance liquid chromatographic method for the separation and determination of process-related impurities of sildenafil was developed. The separation was achieved on a reversed-phase C18 column using acetonitrile-0.05 M potassium dihydrogen orthophosphate (70:30 v/v) as a mobile solvent at a flow rate of 1.0 ml/min and UV detection at 230 nm. The method was used not only for quality assurance, but also for monitoring the chemical reactions during the synthesis of sildenafil. It was found to be specific, precise and reliable for the determination of all process-related impurities of sildenafil in bulk drugs and formulations.     

Base-Catalyzed Synthesis of Spiropyrazoloaminonitriles with Arylidene Pyrazolone and Vinylogous Malononitriles through a Cascade Michael Addition and Cyclization

Synthesis of title compounds were accomplished by a reaction of vinyl malononitriles and arylidene pyrazolones catalyzed by base. This protocol proceeds via Michael addition followed by intramolecular cyclization leading to the formation of two new C−C bonds. Further the same reaction was also conducted with α,α-dicyano olefins and vinyl malononitriles to furnish 1,6-dihydro biphenyl compounds. Simple reaction conditions, high yields and compatibility are the advantages of this protocol.