Mercuration of 2′-deoxyuridine 5′-phosphate (dUMP) followed by alkylation with allylamine in the presence of K2PdCl4 afforded the 5-aminoallyl deoxynucleotide, which was isolated by sequential Dowex 50 H+ and DEAE-Sephadex chromatography. Further reaction of the product with the N-hydroxysucci...

Colorless crystals of 5-(2,5-dimethylphenoxy)-2,2-dimethyl pentanoic acid were grown by slow evaporation method and the FT-IR and FT-Raman spectra of the sample were recorded in the region 4000–450 cm−1 and 4000–50 cm−1 respectively. Molecular structure is optimized with the help of B3LYP/6-31...

The first representatives of 3-trifluoromethyl-2-(dialkoxyphosphoryl)imidazo[1,2-a]pyridines have been synthesized by the reaction of N-(pyridin-2-yl)-perfluoropropanimidoyl chlorides with triethyl phosphite.

A series of novel trifluoromethyl substituted furo[2,3-b]pyridine and pyrido[3′,2′:4,5]furo[3,2-d] pyrimidine derivatives 3a-b, 6a-k, 9, 10a-b, 11a-c and 12a-c were prepared from 2-carbethoxy-3-amino-6-trifluoromethyl furo[2,3-b]pyridine 1 under different set of conditions. Compounds functiona...

2-Amino-3-cyano-4-trifluoromethyl-6-substituted pyridines have been obtained from 3-cyano-4-trifluoromethyl-6-substituted-2(1H)pyridones via an interesting rearrangement of 2-O-acetamido-3-cyano-4-trifluoromethyl-6-sub-stituted pyridine intermediates.

The cyclization of acylated 4-amino-5-aryl-2-(trifluoromethyl)pyridines under the action of P2O5/POCl3 smoothly afforded 3-(trifluoromethyl)benzo[c][1,6]naphthyridines in good yields. Intermediate aminopyridines were synthesized in a two-step sequence from the corresponding 4H-pyran-4-ones, whic...

5-Alkyl-4-amino-2-(trifluoromethyl)pyridines were prepared in good yields starting from the corresponding pyridinols either using condensation with tosyl isocyanate or by alkylation with 2-chloroacetamide and subsequent Smiles type rearrangement. The cyclisation of diazonium salts, generated fro...

A series of novel 3,5-diaryl-1H-pyrazolo[3,4-b]pyridines as tubulin polymerization inhibitors targeting the colchicine site were designed via ring tethering strategy, which was supported by conformational analysis. The general, chemically unstable and rotational linker, carbanyl group, was locke...

Transmetalation reaction between Z-vinylic tellurides and higher order cyanocuprates generated the corresponding Z-vinylic cyanocuprates. Conjugate addition of these cuprates to enones followed by O-functionalization led to silyl enol ethers, vinyl phosphates and vinyl triflates. The vinyl trifl...

Stereoselective synthesis of fluoroalkenes is described. (Z)-2-Fluoro-1-alkenyl(phenyl)iodonium tetrafluoroborates (1) were synthesized stereoselectively in good yields by Michael-type addition of HF to 1-alkynyl(phenyl)iodonium tetrafluoroborates (2) with a commercially available HF reagent, hy...

Reaction of E/Z mixtures of 1-bromo-1-fluoroolefins with 1-alkynes and catalytic Pd(PPh3)2Cl2 and CuI in triethylamine at room temperature gave (after 16–24 h) predominately the (Z)-monofluoroenyne (Z/E>92/8) in good yields. Pure (Z)-monofluoroenyne could generally be obtained by chromatographi...

The Lewis b hexasaccharide, α-l-Fucp-(1→2)-β-d-Galp-(1→3)-[α-l-Fucp-(1→4)]-β-d-GlcpNAc-(1→3)-β-d-Galp-(1→4)-β-d-Glcp, has been synthesised using a convergent synthesis. Starting from ethyl 4,6-O-benzylidene-2-deoxy-2-phthalimido-1-thio-β-d-glucopyranoside, a thioglycoside tetrasaccha...

Na+/K+-ATPase is responsible for maintaining electrochemical gradients of Na+ and K+, which is essential for a variety of cellular functions including neuronal activity. The α-subunit of the Na+/K+-ATPase is composed of four different polypeptides (α1–α4) encoded by different genes. Na,K-ATP...

In this work thermochemistry of solution and solvation of mono- and di-substituted chloro- and nitro-benzenes in 1-butyl-3-methylimidazolium tetrafluoroborate ([BMIM][BF4]), 1-butyl-3-methylimidazolium trifluoromethanesulfonate ([BMIM][TfO]) and 1-butyl-3-methylimidazolium bis(trifluoromethylsul...

A series of symmetrically bis-substituted imidazole analogs bearing at the N-1 and N-3 two biphenyl moieties ortho substituted either with tetrazole or carboxylate functional groups was designed based on docking studies and utilizing for the first time an extra hydrophobic binding cleft of AT1 r...

The reaction of compounds 6a–i, readily available from α-amino acids, with an excess of lithium diisopropylamide, leads to new 3-substituted-2H-1,2-naphthothiazin-4(3H)-one 1,1-dioxides 7a–i, with yields ranging between 21 and 70%. The key steps are: the naphthylsulfonyl ortho-deprotonation b...

Density functional theory (DFT) calculations have been carried out at the hybrid Becke 3-Lee–Yang–Parr; B3LYP/3-21G** level of theory to study two series of hydroxy-chalca-acetic acid-(4-pyrrolidin-1-yl-phenyl) ester [C60-C2H4N-(4-XCOCH2OH)C6H4] and hydroxy-chalcoacetic acid-[2-(2-hydroxy-acet...

The epidermal growth factor receptor represents an important target in cancer therapy, and low molecular weight inhibitors based on quinazolines have reached the marked. Herein we report on a new scaffold, 5-aryl-7H-pyrrolo[2,3-d]pyrimidin-4-amines, and show that when employing (S)-phenylglycino...

New BINOL-derived ligands, 3,3′-bis(2-oxazolyl)-1,1′-bi-2-naphthols (BINOL-Box), bearing chiral bis-oxazoline at the 3,3′-carbons, were synthesized from commercially available 1,1′-bi-2-naphthol (BINOL). With the new ligands obtained, we found that asymmetric 1,3-dipolar cycloaddition reacti...

The reactions of the polydentate ligand 1,4-bis(4,5-dihydro-2-oxazolyl)benzene (L) with AgX (X = CH3COO−, ClO4− and CF3SO3−) afforded the complexes [Ag2(L)(CH3COO)2]∞ (1), [Ag2(L)3(ClO4)2]∞ (2), and [Ag(L)(CF3SO3)]∞ (3), whereas the reaction of L with Ag2SO4 in MeOH/H2O system afforded {[Ag2(...