Department of Applid Chemistry

4-(4-Aminophenyl)-1-thia-4-azaspiro[4.5]decan-3-one 1 was prepared and allowed to react with nitrogen nucleophiles to give the corresponding hydrazones 2–4. Further, compound 1 underwent diazotization and afforded the parallel hydrazono derivative 5; moreover, compound 1 refluxed with active methylene derivatives yielded the corresponding aminospirothiazolo pyridine–carbonitrile derivative 6 and spirothiazolopyridinone–carbonitrile derivative 7. Condensation of spirothiazolidine 1 with 4-chlorobenzaldehyde gave the corresponding spiro arylidiene derivative 8, which was utilized as a component of Micheal addition to react with excess of nitrogen nucleophiles to yield novel ring frameworks 4-(3′-(4-chlorophenyl)–spiro [cyclohexane-1,5′-pyrazolo[3,4-d]thiazol]-6′(1′H)-yl)aniline (9) and 4-(3′-(4-chlorophenyl)-6′H- spiro[cyclohexane-1,5′-thiazolo[5,4-d]isoxazol]-6′-yl)aniline (10). Finally, when spirothiazolo pyridinone–carbonitrile derivative 7 sodium salt generated in situ was reacted...

Reaction of imidazolidineiminothiones with some amino acids methyl ester afforded imidazopyrazine and imidazolidine derivatives. Some of obtained products were synthesized by nano technology; where this method reduces the reaction time significantly. The evaluation of biological activity of some selected compounds was carried out and some of synthesized compounds displayed anticancer activity.

Amino thiophenecarboxylates 1a-d were heated with thiourea to afford 2-thioxothieno[3,2-d]pyrimidin-4(1H)-ones 2a-d. 2-(Methylthio)thieno[3,2-d]pyrimidin-4(1H)-ones 3a-d were synthesized by alkylation of substituted 2-thioxo derivatives 2a-d with methyl iodide. Compounds 3a-d were treated with (2-acetoxyethoxy)methyl bromide to afford 4a-d which were deacetylated to afford 5a-d. The anti-HBV activity of selected compounds was studied.

The present work represents the reaction of different hydrazides with carbon disulfide in the presence of potassium hydroxide to afford 1-(1,3,4-oxadiazol-5-ylmethyl-2-thio)-pyrimidinedione derivatives. Conventional heating and microwave irradiation (MW) of the 1,2,4-triazoles with hydrazine hydrate afforded the corresponding 4-amino-1H- 1,2,4-triazole-5(4H)-thiones. Treatment of the latter compounds either with carbon disulfide in the presence of KOH or with methyl iodide followed by reaction with phthalaldehydic acid under microwave conditions using isopropyl alcohol or dimethylformamide as a solvent afforded the thioxo[1,2,4]triazolo[3,4-b]thiadiazoles and 4-amino-5- (methylthio)-4H-1,2,4-triazoles, respectively. Conventional heating and microwave irradiation (MW) of 4-amino-5- (methylthio)-4H-1,2,4-triazoles with different aromatic aldehyde afforded the corresponding schiffE¹s bases. While reaction of 4-aminotriazoles with phthalaldehydic acid afforded different products dependi...