The Journal of Organic Chemistry (ACS Publications)

The 5-acetyl-derivatives were converted into pyrimido-oxazoles, pyrimido-pyrazoles, and chalcones

The chemistry of isatins: a review from 1975 to 1999 - …

All measurements were done in chloroform as a solvent which has zero inhibition activity. The antimicrobial activity of the tested compounds were examined with gram positive bacteria, Bacillus subtilis, Bacillus cereus and Staphylococcus aureus and gram negative bacteria Escherichia coli, Pseudomonas aeruginose and the fungus Candida albicans. The obtained results are compared with a reference antibiotics that were purchased from Egyptian markets.

Synthesis and studies of chalcones and its Cyanopyridine and Acetyl Pyrazoline Derivatives.

06/06/2014 · Review

Other interesting pyrimidine containing compounds are those derived from dihdropyrimidinones (the so called Biginelli compounds) 5 which draw the attention of many synthetic workers in the last few decades. These compounds even those having small molecules, are known by their antihypertensive properties 6 in addition to their diverse range of biological activities such as antiviral 7, antimicrobial 8, antitumor 9, anti-inflammatory 10 and especially as antifungal activities 11.

General method: A mixture of compound 10 (2.76 g, 10 mmol) and the appropriate secondary amine, namely, piperidine, morpholine or methyl piperazine (10 mmol) and paraformaldehyde (0.99 g, 33 mmol) in absolute ethyl alcohol (50 mL) was heated under reflux for 12 h. (monitored by TLC). The solvent was then evaporated under vacuum and the residue obtained was treated with water, filtered then washed with water, dried and crystallized from methanol to give compounds (19-21)


Synthesis and evaluation of anticancer activity of …

General procedure: To a solution of the appropriate acetyl derivative 1 or 4 (10 mmol) in dioxane (30 mL), was added hydrazine hydrate (2 mL), the mixture was then heated under reflux for several hours until completion of the reaction (monitored by TLC). The solvent was removed under reduced pressure and the residual product was treated with water, filtered, washed with water and dried. Crystallization from methanol gave the title compounds 14 and 15

Combinatorial Synthesis and Antibacterial Evaluation …

General procedure: A mixture of any of the acetyl derivatives 1,3 or 4 (10 mmol), hydroxylamine hydrochloride (1.0 g, 15 mmol) and anhydrous sodium acetate (1.5g) in absolute ethyl alcohol (30 mL) was heated under reflux for several hours until completion of the reaction (4-12 h, monitored by TLC). The solvent was removed under reduced pressure and the residual product was treated with water, filtered,washed with water and crystallized from methanol to give the title compounds 11-13

SYNTHESIS AND ANTIMICROBIAL ACTIVITY OF NEW 3, …

Totally twenty-seven 3,5-substituted-4,5-dihydroisoxazole derivatives 59 (fig. 8) including 3-(2-fuorneyl)-5-(substituted phenyl)-4,5-dihydroisoxazole have been synthesized by fly-ash: H2SO4 catalyzed intramolecular cycloaddition of hydroxylamine hydrochloride and aryl chalcones under solvent free conditions by Ganesamoorthy et al. [54]. The yields of the isoxazoles are more than 90 %. The antimicrobial and antioxidant activities of the synthesized isoxazoles were evaluated using cup plate and DPPH radical scavenging methods, respectively.

and Chalcones , Organic Letters, ..

General procedure: To a solution of any of the acetyl derivatives (1-4) (10 mmol) in ethanol (30 mL), was added 5-methylfurfural (1.1 mL,10 mmol) followed by addition of 30% solution of sodium hydroxide (12 ml). The mixture was stirred at room temperature for 24 h. The reaction product was then diluted with water (250 mL), acidified with dilute HCl and the formed precipitate was filtered, air dried and crystallized from dil. ethanol to give the desired compounds 5-8.