A family of cationic lipids was synthesized via direct amide coupling of spermine to the C-24 position of cholic acid analogs. Four monosubstituted spermines and a bis-substituted spermine were evaluated as plasmid transfection reagents, as bacteriostatic agents, and as bactericidal agents. The incorporation of a double bond in the sterol moiety enhanced transfection efficiency significantly an...

The synthesis of polyethynyl aromatics as starting materials for the preparation of highly cross-linked organic solids containing high atom fractions of carbon is described. Treatment of bromoand iodoaromatic compounds with (trimethylsily1)acetylene (TMSA) in the presence of palladium(0) and copper(1) in amine solvents yields (trimethylsily1)ethynyl-substituted aromatics. The TMS protecting gro...

A novel synthetic methodology for the synthesis of Bis(indolyl)methanes by using catalytic amount of ferric triflate was described Introduction Bis(indolyl)methanes consists two substituted indole units in the molecule. Bis indole derivatives are reported to exhibit a wide spectrum of pharmacological activities such as cytotoxic, antitumor antimicrobial [1] and antiactivities. [2] For the past ...

Singlet oxygen (1O2) proves to be a powerful tool in mediating the one-pot synthesis of a salinomycin-type [6,6,5]-bis-spiroketal unit starting from a suitably substituted furan nucleus.

Microwave-assisted double decarboxylative Claisen rearrangement of bis(allyl) 2-tosylmalonates provides substituted 1,6-heptadienes, which may be alkylated, and then converted into pyridines by ozonolysis followed by reaction with ammonia generated in situ under microwave conditions.

Simple alkyl-substituted pillar[5]arenes can form stable interpenetrated complexes with neutral bis(imidazole) guests utilizing multiple C-H···O(N) hydrogen bond and C-H···π interactions.

2-(Pyridinium-1-yl)-1,1-bis(triflyl)ethanides have been used as 1,2-dipole precursors in a metal-free direct [2+2] cycloaddition reaction of alkynes. Starting from stable zwitterionic pyridinium salts, the electron deficient olefin 1,1-bis(trifluoromethylsulfonyl)ethene is generated in situ and immediately reacted at room temperature with an alkyne to afford substituted cyclobutenes. Remarkably...

The C-C coupling of N,N'-bis(5-norbornene-2,3-dicarboximide) (3) and N,N'-bis(7-oxa-5-norbornene-2,3-dicarboximide) (6) with aryl and heteroaryl iodides gave under reductive Heck conditions the C-aryl(hetaryl), substituted N,N'-bistricyclic imides 7a-f and 8a,b. The fused spiro-1,3-indandionolylpyrrolidine compounds, 9, 10 and 11 were also obtained from ninhydrine, sarcosine and 3 or 6 via [3+2...

The diversified bis-isoquinolinones were obtained in two steps, utilizing homophthalic acid and various acid chlorides providing 3-substituted isocoumarins in the first step which on further condensation with 1,7-heptadiamine involving C-N bond formation from the lactone in the presence of 10 mol% zinc oxide nanoparticles (ZnO NPs) (<150 nm) afforded the desired bis-isoquinolinones in high yiel...

Chiral C(2)-symmetric 3,4-bis-silyl-substituted adipic acid derivatives have been synthesised by a Mg/trimethylsilyl chloride-mediated intramolecular reductive coupling of symmetrical disiloxanes of beta-silylacrylic acid N-oxazolidinone derivatives. Efficient and short syntheses of enantiomerically pure enantiomers of 2,6-dioxabicyclo[3.3.0]octane-3,7-dione have been achieved from the bis-sily...