Tetrazole carboxylic acid bioisosteres of γ-linked dipeptide derivatives of 2-desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid (ICI 198583), a folate-based inhibitor of thymidylate synthase (TS), were synthesised by multistep routes starting from the appropriate pteroic acid analogue and Z...

A synthesis of a tetrafluoro derivative of the quinazoline antifolate 2-desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid is described. 2-Desamino-2-methyl-N10-propargyl-2′,3′,5′,6′-tetrafluoro-5,8-dideazafolic acid (1) has been made in four stages from 4-amino-2,3,5,6-tetrafluorobenzoic...

Two thiophene-based and carbazole-based conjugated microporous polymers (PTPATTh and PTPATCz) with triphenylamine core structural monomers were synthesized via straight forward anhydrous ferric chloride oxidative coupling polymerization. We first explored the fluorescent sensing performance of t...

A range of reported methods have been assessed for the synthesis of two coumarin fluorophores containing azides, 1a and 2, for subsequent “click” modification. In the case of 1a reported methods were successfully applied, but the resulting azide proved to be rather unstable and appears more su...

A facile [3 + 2] cycloaddition / aromatization cascade reaction with broad substrate scopes in up to 94% isolated yield was disclosed herein. This tandem approach was accomplished by employing isoquinolines and bromoacetyl derivatives with methyl perfluoroalk-2-ynoates as readily available start...

The FTIR and FT-Raman spectra of 6-bromo-4-chloro-3-formyl coumarin (6B4C3FC) have been recorded in the region 4000–400 and 4000–100 cm−1, respectively. The optimized geometry, frequency and intensity of the vibrational bands were obtained by the density functional theory (DFT) using 6-31G(d,p...

The vibrational and electronic properties of 2-(bromoacetyl)benzo(b)furan have been studied in the ground state using experimental techniques (FT-IR, FT-Raman and UV) and density functional theory (DFT) employing B3LYP exchange correlation with the 6-31G(d,p) basis set. The theoretically calcula...

In an attempt to arrive at a more potent antitumor agent than the parent natural saponin hederacolchiside A1, 23 hederacolchiside A1 derivatives (4a-4w) were synthesized via Cu(I)-catalyzed azide-alkyne 1,3-dipolar cycloaddition and screened in vitro for cytotoxicity against six human cancer cel...

ObjectiveHederacolchiside A1, exhibits cytostatic and cytotoxic activity against various cancer cells in vitro, however, the mechanism is not well understood.

Two efficient and scalable asymmetric syntheses of C(1)–C(6) fragment of epothilones and their structural analogues from commercially available 1,2:5,6-di-O-isopropylidene-d-mannitol have been performed in seven and 12 steps with 35% and 36% overall yields, respectively. Both the approaches inc...

Milligram quantities of α-D-ribofuranosyl 1-phosphate (sodium salt) (αR1P) were prepared by the phosphorolysis of inosine, catalyzed by purine nucleoside phosphorylase (PNPase). The αR1P was isolated by chromatography in >95% purity and characterized by 1H and 13C NMR spectroscopy. Aqueous so...

A series of cerium modified Silicalite-1 molecular sieves were prepared by incipient wetness impregnation and used as the catalysts in the conversion of methanol to propene (MTP). The cerium modified Silicalite-1 catalysts were characterized by X-ray diffraction (XRD), N2 sorption, pyridine adso...

Homo- and copolymers of propene and 1-undecene were synthesized by controlled olefin polymerization (quasi-living polymerization) using two bis(phenoxyamine) zirconium complexes as catalysts. The controlled character is demonstrated by an asymptotic growth of molar mass as a function of polymeri...

Linear dichroism, fluorescence polarization and quantum-mechanical studies of 9,10,19,20-tetra-n-propylporphycene led to the determination of the absolute directions of transition moments for six electronic transitions. The analysis of the transition moment directions reveals a double minimum ch...

Substitution of 2,7,12,17-tetra-n-propylporphycene by an acetoxy group lifts the degeneracy in two trans tautomeric species which, by symmetry, are identical in the parent compound. Absorption spectra reveal the presence of both tautomers in comparable quantities in the ground electronic state, ...

The synthesis of four novel compounds, (i) [(11-{[2-(3-nitrophenyl)-4-oxo-1,3-thiazolidin-3-yl]amino}-11-oxoundecyl)sulfanyl]acetic acid (4), (ii) N-[5-methyl-2-(3-nitrophenyl)-4-oxo-1,3-thiazolidin-3-yl]undec-10-enamide (5), (iii) 2-[(11-{[5-methyl-2-(3-nitrophenyl)-4-oxo-1,3-thiazolidin-3-yl]a...

In the present communication, a new series of 2-[(phenylmethylene)hydrazono]-4-oxo-3-phenyl-5-thiazolidineacetic acids (2a–p) have been synthesized. Benzaldehyde 4-phenyl-3-thiosemicarbazones substituted (1a–p) were also obtained and used as intermediate to give the title compounds. All synthe...

Commercial polyamide (PA) reverse osmosis (RO) membranes were surface modified in a sequential two-step polymerization process to impart anti-biofouling properties to the membrane surface. In the first step, a 2-bromoisobutyryl bromide initiator-polydopamine (BiBBr-initiator-PDA) layer was depos...

The technically important α-methoxylation of aliphatic ethers and acetals to form mixed acetals respectively aldehydes or ortho-esters can be performed electrochemically at low potentials in methanol solution using an undivided cell and tris(2,4-dibromophenyl)amine as redox catalyst. The regios...

Publisher SummaryThis chapter discusses the analytical profile of thiamine hydrochloride. Its generic names are thiamine hydrochloride and vitamin B1. Its trade names are vitamin B hydrochloride, thiamine chloride hydrochloride, aneurine hydrochloride, and thiaminium-chloride. Its molecular weig...