Hamed A. Derbala

CONVERSION OF 3-ARYL-5-PHENYL-2(3H)-FURANONES INTO 3(2H)-ISOTHIAZOLONE DERIVATIVES

Abstract Upon heating 3-aryl-S-phenyl-2(3H)-furanones (la-c) with benzylamine at 100°C in the absence of solvents, ring opening occurred with the formation of the corresponding N-benzylamides (3a-c). When the latter compounds (3a-c) were allowed to react with thionyl chloride at room temperature, the corresponding isothiazolones (4a-c) were obtained. Treatment of the isothiazolones (4a-c) with sodium hydroxide in benzene at room temperature affected debenzoylation to give the corresponding 2-benzyl-4-aryl-3(2H)-isothiazolones (5a-c).

HETEROANNULATED QUINAZOLINE AND QUINAZOLINONE DERIVATIVES FROM (Z)-2-[1-BENZAMIDO-2-(3,4,5-TRIMETHOXYPHENYL)] VINYL-3,1-BENZOXAZIN-4(3H)-ONE

The title compound 1 was prepared and allowed to react with a series of nitrogen nucleophiles to afford the quinazoline and quinazolinone derivatives 2–12 and tetrazole derivative 13. The IR, 1H NMR, 13C NMR, and mass spectra of all the synthesized compounds were discussed.

Synthesis and spectral characterisation of some phthalazinone derivatives

1,2,4-Triazol-3-yl, 1,3,4-oxadiazol-2-yl, 1,3-dioxoisoindolin-2-yl, 1H-pyrazol-4-yl, phthalazin-1(2H)one, 5H-2,3-benzodi-azepine-1,4-dione and pyridazine-1,4-dione derivatives were prepared via the reaction of the readily obtainable starting material 1-oxo-1,2-dihydrophthalazin-4-carbohydrazide with one carbon donor like phenyl isothiocyanate, phenyl isocyanate, triethylorthoformate, formic acid and different electrophilic reagents such as anhydrides, chromen-1,3-dione, chloroacetyl chloride, acetic anhydride, arylidene malononitrile, ethoxymethylene malononitrile and ethyl acetoacetate.

Synthesis and Some Reactions of 4-Aroyl-3-Chloro-6-p-Tolylpyridazines

Abstract 4-Aroyl-3-chloro-6-p-tolylpyridazines (3a &b) were prepared by the action of phosphorous oxychloride on (2). (3a &b) react with hydrazine hydrate to give the pyrazolinopyridazines (4a &b) and with hydroxylamine hydrochloride to give the isoxazolopyridazines (7a &b), respectively. (4b) was also synthesized by the action of phosphorous oxychloride on the hydrazone (5). The reaction of (3a &b) with primary amines in boiling ethanol gives (8a-e), while their reaction with primary aromatic amines in the presence of solvent gives the Schiffs bases (9a-c).

SYNTHESIS AND SOME REACTIONS OF 4-AROYL-6-ARYL PYRIDAZIN-3(2H)-THIONES

Abstract 4-Aroyl-3-chloro-6-aryrylpyridazines[1] (1) react with thiourea to give 4aroyl-6-arylpyri-dazin-3 (2H)-thiones (2) respectively[2–7]. The compounds 2 reacted with dimethyl sulphate, hydrazine hydrate and hydroxylamine hydrochloride to give 4-aroyl-6-aryl-3-metylthiopyri-dazines 5, pyrazolinopyridazines 7 and isoxazolopyridazine 8, respectively. The compounds 2a-c reacted in alkaline ammonium hydroxide solution with sodium hypochlorite solution to give the isothiazolopyridazines 10a-c.

Reaction of N-Arylcitraconisoimidium Perchlorates with Aromatic Hydrocarbons Under Friedel-Crafts' Conditions, a New and Convenient One-Step Method for the Synthesis of β-Aroyl-α-aryl-N-arylbutyramides

Abstract A number of β-Aroyl-α-aryl-N-arylbutyramides (4a-h) have been synthesized using a new methodology involving arylation at the A,β-unsaturated ketonic systems of N-aryl-citraconisoimidium perchlorates (2a-c), followed by a subsequent ring opening via addition on the carbonyl group to give the title compounds (4a-h).