Organic Communications Articles

In a heretofore-unreported reaction, 1,2-cyclohexandione reacts with a variety of alcohols under mild acid-catalyzed dehydration conditions to afford not only ethers of 1,2- cyclohexanedione but the corresponding aryl ethers as well in moderate to good yield.

A synthetic methodology for preparation of β-cyano-ʟ-alanine was developed via ʟ -serine. Esterification of ʟ -serine with MeOH, followed by protection of NH 2 with CBz, gave methyl 2-(benzyloxycarbonylamino)-3-hydroxypropanoate. Mesylation of OH group, and then cyanation, ester hydrolysis and removal of the CBz group with catalytic hydrogenation, gave β-cyano-ʟ-alanine. Crucial step for the synthesis of the title compound was cyanation with K 13CN.

The oxidation reaction of ferrocene derivatives is important because of its biological applications. The reactivity is affected by metal ions. However, it is not clear how to interact the metal ions with the ferrocenes. In this paper, the oxidation reactivity of (o-acetylphenyl)ferrocene was investigated in the view of solvent effect and the addition effect of salicylic acid. Furthermore, the measurement of the relaxation time was carried out. As a result, Al 3+ would strongly interact with (o-acetylphenyl)ferrocene so that prevent the mobility of the acetyl group.

Carbonic anhydrase inhibitors are both in clinical use as antiglaucoma, diuretics, antiepileptics and management of altitude sickness, and under investigation as anticancer, anticonvulsant and antiobesity agents. Sulphonamides have been known for decades as carbonic anhydrase inhibitors and are in clinical use. Sulphonamide derivatives of p-hydroxybenzoic acid and 3,4,5-trihydroxybenzoic acid (gallic acid) were synthesized and their inhibition values over hCA I and hCA II isozymes, purified from human erythrocyte cells by Sepharose-4B-L-tyrosine-sulphanilamide, were determined. Compounds synthesized showed efficient carbonic anhydrase inhibition activity at low nM levels.

A novel series of Schiff bases derivatives containing the benzothiazolone moiety have been synthesized in a simple and efficient method, by condensation of 6- amino-2(3H)-benzothiazolone substrates with different aromatic aldehydes, in refluxing ethanol and in the presence of acetic acid as catalyst. The structure of synthesized compounds was elucidated and has been proven using spectral methods such as 1 H NMR, 13C NMR and elemental analysis . All the newly synthesized compounds were in good agreement with the proposed structures.

The synthesis of 2-amino chromene, reported in our previous paper, has been accomplished by the reaction of cyanoiminocoumarin and β-naphthol . The obtained compound was reacted   with various electrophilic or nucleophilic reagents. All the new homologous 2-amino-4H-chromenes have been characterized on the basis of their spectral (IR, 1H and 13C NMR) data and microanalysis. Four compounds were evaluated   in vitro  for their preliminary antibacterial activities against five different pathogenic bacterial strains such as Bacillus thuringiensis , Escherichia coli , Staphylococcus aureus, klebsiella pneumonia and Salmonella Sp . Antibacterial activity of each compound was compared with standard drug, Penicillin.

A simple and efficient method for the synthesis of biotin pre-functionalized linkers via orthogonal protecting group elongation strategy is reported for a single-step preparation of new biosensor probes. The target compound 4- (4- (4- (5- ((3S, 4S, 6R)-2-oxohexahydro-1H-thieno[3,4]imidazol-4-yl) pentanamido) butanamido) butanamido) butanoic acid (5) was synthesized in five linear steps with a 40% overall yield.

A simple and efficient synthesis of bis(α-aminophosphonates) has been developed by the reaction of aromatic aldehydes, 1,4-phenylenediamine and diethylphosphite in the presence of cellulose-SO 3H as catalyst under neat conditions at room temperature for 10-30 minutes. The synthesized compounds were screened for their antioxidant activity against DPPH, NO and H 2O 2 scavenging methods. All the compounds exhibited good to moderate activity.