Table of Contents

Abstract: n/a

Abstract: The protected 2-formyl-L-arabinal 2 reacted with thiourea and cyanamide in the presence of sodium hydride to afford via ring transformations the 5-[1R,2S-1,2- bis(benzyloxy)-3-hydroxypropyl]-1,2-dihydropyrimidines 3 and 4, respectively. Similarly, treatment of 2 with 3-amino-2H-1,2,4-triazole yielded 6-[1R,2S-1,2- bis(benzyloxy)-3-hydroxypropyl][1,2,4]-triazolo[1,5-a]pyrimidine (5).

Abstract: Triisobutylaluminium-promoted rearrangement of unsaturated glycosides containing electron-donating aglycons, such as C-aryl glycosides, provides direct access to highly functionalised cyclohexane derivatives.

Abstract: Epoxidation and cis-hydroxylation of C-phenyl-∆^2,3-glycopyranosides have beencarried out with a view to developing C-aryl glycoside synthesis. Epoxidation of (2,3- and (6-O-tert-butyldimethylsilyl-2,3-dideoxy-D-erythro-hex-2-enopyranosyl)benzenedideoxy-D-erythro-hex-2-enopyranosyl)benzene gave predominantly the allo-adductswhatever the configuration at the anomeric center. Epoxidation of (4,6-di-O-tert-butyl-dimethylsilyl-2,3-dideoxy-D-erythro-hex-2-enopyranosyl)benzene gave the manno- andallo-adducts in a 89:11 and 40:60 ratios for the α- and β-anomers, respectively.Hydroxylation of α-C-phenyl-∆^2,3-glycopyranosides using OsO4 afforded the manno-adductonly, whatever the substituents at positions 4 and 6, whereas hydroxylation of (2,3-dideoxy-β-D-erythro-hex-2-enopyranosyl)benzene and (4,6-di-O-tert-butyldimethylsilyl-2,3-dideoxy- β-D-erythro-hex-2-enopyranosyl)benzene gave the manno- and allo-adducts in25:75 and 80:20 ratios, respectively.

Abstract: Application of the Ferrier rearrangement led to a novel carbohydrate based synthetic route to 4-aminohexenoic acid viz. (R) and (S)-vigabatrin. The potential of D- glucose or D-galactose as the chiral starting materials for the synthesis of (R) and (S)- vigabatrin has been explored.

Abstract: Bi(OTf)₃ and SiO₂-Bi(OTf)₃ are found to effectively catalyze the Ferrierrearrangement of tri-O-acetyl glycals with different alcohols providing an effective routeto 2,3-unsaturated O-glycosides with good anomeric selectivity and good to excellentyields after short reaction times.

Abstract: The intramolecular aminomercuration of γ-alkenylamines 1a, 1b and 4 was shown to afford the 5-endo-trig cyclized product exclusively in good yield. The utility of pyrrolidine derivatives thus obtained from D-glucose derived γ-alkenylamines 1a and 1b was demonstrated in the synthesis of 1-deoxycastanospermine (3a) and 1-deoxy-8a-epi- castanospermine (3b).

Abstract: Cyclophellitol and its C3-epimer have been synthesized from5-enoglucopyranoside and 5-enomannopyranoside, respectively. The carbocyclic skeletonwas constructed through a Ferrier-II reaction meditated by PdCl₂.

Abstract: A new iso-amyl benzothiazolyl sulfoxide (ABSO) was synthesized and used inthe extraction of Pd(II) from hydrochloric acid media. Pd(II) was extracted quantitativelyfrom 0.1 M HCl with ABSO in benzene (0.5 M). Ammonia solution (2.0 M) could beused as stripping agent. ABSO and Pd(II) form a 2:1 adduct [Pd (ABSO)₂Cl₂] in theextraction. X-ray crystal structure determination revealed PdCl₂(ABSO)₂ is asquare-planar complex in which ABSO acts as a neutral unidentate ligand coordinatedwith palladium(II) via the thiazolyl N atom.

Abstract: The present study examined the influence of synthetic N-(1,3-benzothiazol-2-yl)-N-(4,5-dihydro-1H-imidazol-2-yl) amine (2-Amdz) on levels of vitamins A, E and C and malondialdehyde (MDA) in rats. A total of 30 rats, divided into two groups, were used in the study. The control group was given only a subcutaneous injection of 250 ?L 75% ethanol, every other day. The other group of rats was administered a subcutaneous injection of 2-Amdz (25 mg kg-1, dissolved in 250 ?L of 75% ethanol). Injections were continued for 16 days. After the application of 2-Amdz for 16 days, the serum levels of vitamins A, E and C and malondialdehyde (MDA) were determined by HPLC. The serum vitamin A, E, and C levels decreased significantly compared to controls (p<0.05) whereas serum MDA levels were higher than control levels (p<0.005). As a result, it can be suggested that 2-Amdz induced a severe stress and more importantly, increased the amount of free radicals and significantly decreased the levels of serum antioxidant vitamins.

Abstract: The syntheses in good yields of some new difunctionalized 1,8-naphthyridines 4, 6, 8 and 9 and a novel triethylene glycol ether-linked dinaphthyridine, 10a, along with the mononaphthyridine-linked ether alcohol 10b are described. An improved and milder method for the synthesis of 2,7-diamino-1,8-naphthyridine (14) is also reported.

Abstract: This review presents a survey of the condensations of 3-formylchromone with various active methylene and methyl compounds, e.g. malonic or barbituric acid derivatives, five-membered heterocycles, etc. The utilisation of the condensation products for the synthesis of different heterocyclic systems, which is based on the ability of the γ-pyrone ring to be opened by the nucleophilic attack is also reviewed. Finally, the applications of microwave irradiation as an unconventional method of reaction activation in the synthesis of condensation products is described and the biological activity of some chromone derivatives is noted.

Abstract: The synthesis of 3-alkyl(aryl)-4-(3-ethoxy-4-hydroxybenzylidenamino)-4,5-dihydro-1H-1,2,4-triazol-5-ones 3 from the reactions of 3-alkyl(aryl)-4-amino-4,5-dihydro-1H-1,2,4-triazol-5-ones 2 with 3-ethoxy-4-hydroxybenzaldehyde is described.The acetylation and methylation reactions of the compounds 3 giving compounds of type4 and 5, respectively, were investigated. The newly synthesized compounds werecharacterized using elemental analyses and IR, ¹H-NMR, ¹³C-NMR and UV spectral data.In addition, to investigate the effects of solvents and molecular structure upon acidity,compounds 3 were titrated potentiometrically with tetrabutylammonium hydroxide infour non-aqueous solvents (isopropyl alcohol, tert-butyl alcohol, acetonitrile and N,N-dimethylformamide). The half-neutralization potential values and the corresponding pKavalues were determined for all cases.

Abstract: A new diacetyl triterpene lactone, drosericarpone (2), was isolated from the hexane extract of the herb Cleome droserifolia, together with buchariol (1, a sesquiterpene oxide, isolated for the first time from Cleome species) and stigmasterol glucoside (3). The structures of 1-3 were identified by spectroscopic means.

Abstract: In this paper we elected to nitrate p-xylene because this compound has onlyone mononitro- and trinitro- isomer. Trinitro-p-xylene was used as a starting material forthe synthesis of other compounds in subsequent work. The mononitration of p-xylene canbe easily carried out at 30°C. Nitro-p-xylene is easily nitrated to dinitro-p-xylene at atemperature of 80°C. The trinitro-p-xylene can be obtained at 120°C. Single crystals of2,3-dinitro-p-xylene and 2,3,5-trinitro-p-xylene were grown using theslow cooling method and we report the X-ray structure of the former. The thermaldecomposition of the compounds was studied using differential scanning calorimetry(DSC) and thermogravimetry-derivative thermogravimetry (TG-DTG) techniques andFT-IR. The target compounds were also characterized by ¹H-NMR, ¹³C-NMR and MS.

Abstract: 4'-(2,6,6-Trimethyl-2-cyclohexen-1-yl)-3'-buten-2'-ketoxime-N-O-alkyl ethershave been synthesized starting from α-ionone, separated into their E and Z isomers andcharacterized on the basis of ¹H-NMR and mass spectra.

Abstract: Some new (naphthalen-1-yl-selenyl)acetic acids derivatives 7a-d have been synthesized by two different methods, using naphthylselenols or naphthylselenocyanates. The structures of the products were investigated by spectroscopic methods.

Abstract: Incubation of sclareol with Rhizopus stolonifer affords in high yield a mixture of triols with 18-hydroxy-sclareol as the main component.

Abstract: Studies aimed at a comparison of chemical, biomimetic (Gif system GoAgg^III)and enzymatic (CHMO) transformations of natural ( )-10β,14-dihydroxy-allo-aromadendrane have led to preparation of an eight-member sesquiterpene lactone.

Abstract: 6-Methylpurine-β-D-riboside (β-D-MPR) has been synthesized by coupling6-methylpurine and 1-O-acetyl-2,3,5-tri-O-benzoyl-D-ribose using conditions that producethe β-D-anomer exclusively. The in vitro antitumor effects of β-D-MPR and 6-methyl-purine-α-D-riboside (α-D-MPR) in five human tumor cell lines showed that β-D-MPR washighly active (IC₅₀ values ranging from 6 to 34 nM). α-D-MPR, although less active than β-D-MPR, also exhibited significant antitumor effects (IC50 values ranging from 1.47 to 4.83"µ"M).