Purple-coloured, tetra-coordinated Ni(II) complexes, Ni[S2P(OR)2]2 (R = o-, m-, p-OC6H4Me, Ph and CH2Ph) have been obtained by reaction of NiCl2 with salts of corresponding O,O′-diaryl(dibenzyl) dithiophosphates and have been characterized by elemental analysis, UV, IR, 1H, and 31P NMR spectros...
Reactions of glutathione (GSH) with O,O-diorganyl dithiophosphoric acids (DTPA) were studied to develop bioactive derivatives of GSH. Effective coupling reaction of GSH with DTPA was proposed to produce the ammonium dithiophosphates (GSH–DTPA) between the NH2 group in γ-glutamyl residue of GSH...
Reactions of dichlorodioxobis(triphenylphosphine oxide)molybdenum(VI) complexes with ammonium/sodium salts of O,O-dialkyl(alkylene) and diphenyl dithiophosphoric acids in 1:1 molar ratio in dichloromethane solution yield dioxomolybdenum complexes of the types, MoO2Cl[S2P(OR)2] · OPPh3 (R=Me, Et...
A carbon-11 labeled methoxyl analog of CP-101,606, (±)threo-1-(4-hydroxyphenyl)-2-[4-hydroxy-4-(p-[11C]methoxyphenyl)piperidino]-1-propanol [(±)[11C]1], was synthesized as a new subtype-selective PET radioligand for NMDA receptors. The in vitro binding studies using rat brain slices demonstrat...
In finding that 2-(4-benzyl-piperidino)-1-(4-hydroxyphenyl)-1-propanol (BPHPP) produced high concentrations of blood glucose in rats, it was observed that (1) the maximum concentration of blood glucose was obtained 1 hr after oral administration at a dose of 100 mg/kg of BPHPP, (2) that BPHPP ha...
A series of N-protected 1-substituted homotaurines was synthesized efficiently from various olefins with O-ethyl S-2-phthalimidomethylxanthate as a sulfur-aminomethylation reagent via a radical addition and subsequent performic acid oxidation. The current method is a convenient and practical met...
Optically active 2-(4-toluenesulfonyloxy)- and (4-nitrobenzenesulfonyloxy)nitriles (R)-3 and (R)-4, which were obtained from (R)-cyanohydrins (R)-2 by sulfonylation, react with sulfur nucleophiles such as potassium thioacetate, potassium ethylxanthogenate, potassium thiocyanate, as well as thioa...
The optimized molecular structure, vibrational frequencies, corresponding vibrational assignments of 5-tert-Butyl-6-chloro-N-[(4-(trifluoromethyl)phenyl]pyrazine-2-carboxamide have been investigated experimentally and theoretically using Gaussian09 software package. Potential energy distribution...
Sixteen 5-aryl-substituted isothiazol-3(2H)-one-1,(1)-(di)oxide analogs have been prepared from the corresponding 5-chloroisothiazol-3(2H)-one-1-oxide or −1,1-dioxide by a Suzuki-Miyaura cross-coupling reaction and screened for their inhibition potency against four human carbonic anhydrase isoen...
Practical synthesis of (±)-α-alkylserines and tert-butyl benzamidoacrylate from tert-butyl 2-phenyl-2-oxazoline-4-carboxylate (6) were developed. The α-alkylation and β-elimination of 6 are dramatically dependent upon base conditions. The phase-transfer catalytic condition bearing solid KOH ...
Due to steric promotion of CH bond activation, the direct ortho-palladation of (S)-4-tert-butyl-2-phenyl-2-oxazoline using Pd(OAc)2 in AcOH provided (S,S)-di-μ-acetatobis-[2-(2-(4-tert-butyl)oxazolinyl)phenyl-C,N]dipalladium(II) (2) in an excellent yield. This complex was converted into its c...
A novel fluorinated diamine monomer with the tert-buty group, 4-tert-butyl-[1,2-bis(4-amino-2-trifluoromethylphenoxy)phenyl]benzene (2), was prepared through the nucleophilic substitution reaction of 2-chloro-5-nitrobenzotrifluoride with 4-tert-butylcatechol in the presence of potassium carbonat...
The piperazine derivatives correspond to an extensive chemical class of compounds with numerous neuropharmacological activities, including antidepressant (e.g., nefazodone, trazodone) and anxiolytic (e.g., buspirone) properties. Therefore, aiming to identify a new antidepressant and antianxiety ...
The cothermolysis of benzoyl(tert-butyl)bis(trimethylsilyl)silane with 2,3-dimethylbutadiene in a sealed tube at 140 °C for 24 h afforded cis- and trans-1-tert-butyl-4,5-dimethyl-2-phenyl-2-(trimethylsiloxy)-1-(trimethylsilyl)-1-silacyclohex-4-ene (2 and 3) in a ratio of approximately 1:1 in 66...
4-(((3-(tert-Butyl)-(1-phenyl)pyrazol-5-yl)imino)methyl)phenol (4-OHFPz) was synthesized and characterized by FT-IR, MS, NMR, and single-crystal X-ray diffraction. Optimization of molecular geometry, vibrational frequencies, and chemical shifts were calculated by using the methods of density fun...
The (tert-butyl isocyanide)(5,10,15,20-{tetrakis-[4-(benzoyloxy)phenyl]porphyrinato}iron(II) coordination compound with the formula [FeII(TPBP)(t-BuNC)2] (I) was prepared by the reduction of the triflato iron(III) starting material [FeIII(TPBP)(SO3CF3)] using a large excess of tert-butyl isocyan...
A new and mild synthetic approach for the synthesis of N-arylsulfonamides under copper-catalyzed conditions at room temperature has been developed. The reaction employs various tert-butyl N-sulfonylcarbamates and diaryliodonium salts to avoid potential genotoxic impurities. A one-pot coupling/Bo...
Racemic 2,3-diphenylbutane-1,4-diol (±)-1 is resolved to obtain the corresponding (R,R)-isomer in 98% e.e. through reaction with (S)-proline and boric acid. Partially resolved (R,R)-(−)-1 and (S,S)-(+)-1 have been enriched to obtain samples of 95 and 97% e.e. through reaction with (S)-proline a...
The aim of this work was to develop an easy and reproducible colorimetric quantitative analysis for residual ethylene oxide after sterilization. The technique proposed is original and uses 4-(p-nitrobenzyl) pyridine. The rapidity and cheapness of the method pleads in favour of its further valida...
6-O-(2-Nitrobenzyl)guanosine and 4-O-(2-nitrobenzyl)uridine triphosphates (NBGTP, NBUTP) were synthesized, and their biochemical and photophysical properties were evaluated. We synthesized NBUTP using the canonical triphosphate synthesis method and NBGTP from 2′,3′-O-TBDMS guanosine via a trip...
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