Green Synthesis of 1-Aryl-2,3,4,9-Tetrahydro-1H-B-Carbolines using Fe(Iii)-Montmorillonite and Study of their Antimicrobial Activity

A series of 1-aryl-2,3,4,9-tetrahydro-1H-_-carbolines were synthesized using green ultrasonic synthetic approach in aqueous medium via the Pictet-Spengler reaction. The condensation reaction of tryptamine and various aromatic aldehydes at 80oC in aqueous medium produced the corresponding 1-aryl-2,3,4,9-tetrahydro-1H-β-carbolines by means of heterogeneous catalysis with Fe(III)-montmorillonite catalyst. The driving force for reaction feasibility in terms of the condensation of β-arylethylamine with the corresponding aldehyde followed by the ring closure reaction is the acidic nature of the Fe(III)-montmorillonite catalyst. The advantage of this methodology is high product yield and short reaction time compared to the conventional heating and microwave irradiation methods. The structures of synthesized compounds were confirmed by IR, 1H and 13C NMR spectroscopy, mass spectrometry, and elemental analysis. All products were screened for their antimicrobial activity, and some compounds exhibited significant activity against selected bacteria and fungi

A simple and convenient protocol for the synthesis of seven- and eight-membered phosphorus heterocycles

<p>A simple procedure for the synthesis of eight-membered 6-(2-chloroethyl)/bis(2-chloroethyl)-amino-12-oxo-dibenzo[d,g][1,3,2]dioxaphosphocin 6-oxides (<b>3a–b</b>) and seven-membered 6-(2-chloroethyl)/bis-(2-chloroethyl)aminodibenzo[d,f][1,3,2]dioxaphosphepin 6-oxides (<b>5a–b</b>) from cyclocondensation of equimolar ratios of 2,2′-dihydroxybenzophenone (<b>1</b>) and 2,2′-dihydroxybiphenol (<b>4</b>), respectively with 2-chloroethylphosphonicdichloride (<b>2a</b>) and bis(2-chloroethyl)phosphoramidic dichloride (<b>2b</b>) in dry toluene in the presence of triethylamine at 45–50 °C is described. All synthesized compounds possessed significant growth inhibition for their antibacteria against ‘Bacillus subtilis’ and ‘Klebsiella pneumonia’ and antifungi activity on “Curvularia lunata” and “Aspergillus niger.”</p

Solvent-free synthesis of α-aminophosphonates: Cellulose-SO3H as an efficient catalyst

α-Aminophosphonates possess a broad range of applications ranging from agrochemistry to medicine. We developed an efficient and eco-friendly Cellulose-SO3H catalyzed one-pot synthesis of α-aminophosphonates by three-component, room temperature reaction of an aldehyde, an amine and dialkylphosphite under solvent-free conditions. The major advantages of the present method are simple experimentation, use of inexpensive and eco-friendly reusable catalyst with good yields and short reaction times

Polyethylene glycol (PEG-400): An efficient medium for the synthesis of 1,2-disubstituted benzimidazoles Polyethylene glycol (PEG-400): An efficient medium for the synthesis of 1,2-disubstituted benzimidazoles

Abstract: Polyethylene glycol (PEG-400) was found to be an inexpensive, non-toxic, and effective medium for the one-pot synthesis of 1,2-disubstituted benzimidazoles in excellent yields. Eco-friendliness, low cost, high yields, and recyclability of the PEG-400 are the important features of this protocol

Palladium-Catalyzed Regioselective Domino Cyclization of Cyclohexadienones

A mild and efficient Pd-catalyzed arylative domino carbocyclization of cyclohexadienone-containing 1,6-enynes is described. The reaction tolerates a variety of functionalized boronic acids to afford a <i>cis</i>-fused bicyclic framework containing an α,β-unsaturated ketone with excellent regio- and diastereoselectivity in good yields. The tandem process proceeds with β-arylation of propargylic ether followed by conjugate addition of a vinyl palladium intermediate and subsequent protonolysis of a palladium enolate

Triton X-100 catalyzed synthesis of α-aminophosphonates

Synthesis of α-aminophosphonates by a three-component condensation of an aldehyde, amines and dialkyl phosphites in the presence of a non-ionic surfactant Triton X-100 catalyst at 70 °C in aqueous medium is accomplished. The advantages are high yield, mild reaction conditions, simple work-up and eco-friendliness. All the newly-synthesized compounds (4a–j) exhibited moderate in vitro antibacterial and antifungal activities