In the present work, 9-fluorenone-2-carboxylic acid methyl ester (1) was prepared from 9-fluorenone-2-carboxylic acid and then converted into the acid hydrazide (2). Compound (2), is the key intermediate for the synthesis of several series of new compounds such as substituted 1,3,4-oxadiazole derivatives (3-6) were synthesized from the condensation of different substituted benzoic acids with compound (2) using POCl3 as condensing agent. Treatment of compound (2) with formic acid gave the N-formyl hydrazide (7), which upon refluxing with phosphorous pentoxide in benzene yielded the corresponding 5-(9-fluorenone-2-yl)-1,3,4-oxadiazole (8). Reaction of hydrazide (2) with phenyl isocyanate to give N-phenyl semicarbazide derivative (9), then this compound (9) convert to 5-(9-fluorenone-2-yl)-N-phenyl-1,3,4-oxadiazole-2-amine (10) via intramolecular cyclization by syrup H3PO4. Also the hydrazide (2) was treated with CS2/KOH afforded 5-(9-fluorenone-2-yl)-1,3,4-oxadiazole-2-thiol (11). Compound (11) was used to react with various alkyl halides and secondary amines to give 5-(9-fluorenone-2-yl)-1,3,4-oxadiazole-2-alkyl thiol (12-15) and 5-(9-fluorenone-2-yl)-1,3,4-oxadiazole-2-N-alkyl (16-19) derivatives respectively.
Two series of bent and liner core mesogen containing 1,2,4-traizole ring [VI]a,g and series were synthesized by many steps starting from esterification of isophthalic acid and terephathalic acid with methanol to yield diester compound [I]a,b which was converted to their acid hydrazide [II]a,b and the acid hydrazide reacted with ammonium thiocyanate or diester reacted with thiosemicarbazide to yield compounds [III]a,b. Then cyclization by 4% NaOH to yielded 1,2,4 traizole-3- thiol compounds [IV]a,b , afterword adding hydrazine hydrate to yield compounds [V]a,b. These compounds condensated with different substituted aldehyde to give new Schiff bases[VI]a,b ,[VII]a,b . Also , reaction acid hydrazide [II]a,b with aldehyde [VII] to yielded Schif
... Show MoreThe work involves synthesis of new quinolin-2-one Schiff bases (XIII)a,b and (XIV)a,b, pyrazoles (XI)a,b and pyrazolines (XII)a,b derivatives containing isoxazoline or pyrimidine cycle starting with chalcones. 3-Aminoacetophenone was reacted with 4-bromobenzaldehyde or 4-N,N-dimethyl aminobenzaldehyde in basic medium to give chalcones (I)a,b by Claisen-Schemidt reaction. These chalcons were reacted with hydroxylamine hydrochloride or with thiourea in basic medium to form isoxazolines (II)a,b or pyrimidine-2-thion (III)a,b ,respectively.Also the pyrimidine-2-thiones (III)a,b and isoxazolines (II)a,b reacted with 4-or 3-substituted benzaldehyde and coumarin to form Schiff bases (IV)a-f (V)a-f and quinoline derivatives (VII)a-d(VIII)a-d, re
... Show MoreTwo new Schiff bases (S1,S2) derived from 2-Amino-2-deoxy chitosamine and mnitrobenzaldehyde
(S1), and with salicylaldehyde (S2) were prepared and
characterized using FTIR, UV and mass spectrometry. New complexes of the
transition metal ions Co (II), Ni (II), Pd (II), Pt (II) with the two ligands were
synthesized and their structures were elucidated depending on atomic absorption,
FTIR, UV-visible spectra in addition to magnetic susceptibility and electrical
conductivity measurement. Metal to ligand [M: L] ratio was obtained for all
complexes in ethanol using molar ratio method, which gave comparable results with
those obtained for the solid complexes. Stability constant of the complexes were
determined using s
A series of Schiff base-bearing salicylaldehyde moiety compounds (1-4) had been designed, synthesized, subjected to insilico ADMET prediction, molecular docking, characterization by FT-IR, and CHNS analysis techniques, and finally to their Anti-inflammatory profile using cyclooxygenase fluorescence inhibitor screening assay methods along with standard drugs, celecoxib, and diclofenac. The ADMET studies were used to predict which compounds would be suitable for oral administration, as well as absorption sites, bioavailability, TPSA, and drug likeness. According to the results of ADME data, all of the produced chemicals can be absorbed through the GIT and have passed Lipinski’s rule of five. Through molecular docking with PyRx 0.8, these
... Show MoreSix transition metal complexes of Cr (III), Mn(II), Co(II), Ni(II), Cu(II), and Zn(II) were prepared using 1,2-bis -(4-Amino-2,3-dimethyl-1- phenyl-pyrazolinyl)-diimino ethane(L) as ligand. These complexes were characterized by elemental analysis, magnetic susceptibility, UV/VIS and FT-IR spectroscopy. These data showed that the solid complexes of Mn(II), Co(II), Zn(II) were tetrahedral geometry, and Cr(III) was octahedral while the symmetry around Ni(II) and Cu(II) ions with the new ligand were square planar of the formula [ML]Cl2 , M=Ni(II) and Cu(II).
A simple method for the determina
... Show MoreA new derivatives of Schiff bases connected with 5H-thiazolo[3,4-b][1,3,4]thiadiazole ring 5a-c were prepared via many reactions starting by treating 1,4-phenylene diamine 1 with chloroacetylchloride to prepared compound 2, then reaction with p-hydroxybenzaldehyde to synthesize compound 3 then, this was reacted with thioglycolic acid and thiosemicarazide to giveN,N-(1.4-phenylene)bis(2-(4-(2-amino-5Hthiazolo[4,3-b][1,3,4]thiadiazol-5-yl)phenoxy)acetamide) 4. Compound 4 was treated with different aromatic aldehydes to give a new derivatives of Schiff bases containing 5H-thiazolo[3,4-b][1,3,4]thiadiazole ring 5a-c. The synthesized compounds were characterized using FTIR spectrophotometer and 1H NMR spectroscopy and the biological activity of
... Show MoreNew series of 2-mecapto benzoxazole derivatives (1-20) incorporated into fused to different nitrogen and suphur containing heterocyclic were prepared from 2-meracpto benzoxazole, when treated with hydrazine hydrate to afford 2-hydrazino benzoxazol (1). Compound (1) converted to a variety of pyridazinone andphthalazinone derivatives (2-4) by reaction with different carboxylic anhydride. Also, reaction of (1) with phenyl isothiocyanate and ethyl chloro acetate afforded 3-phenyl-1,3-thiazolidin-2,4-dione-2-(benzoxazole-2-yl-hydrazone) (6). Azomethines (7-10) were prepared through reaction of (1) with aromatic aldehyde, then (7, 8) converted to thaizolidinone derivatives (11, 12). Treatment of (1) with active methylene compounds afforded deriva
... Show MoreNew 1,2,4-triazole derivatives of 2-mercaptobenzimidazole (MB) are reported. Ethyl (benzimidazole-2-yl thio) acetate (1) has been prepared by condensing 2-mercaptobenzimidazole with ethylchloroacetate. The ester (1) on reacting with hydrazine hydrate gave the corresponding acetohydrazide(2)which was reacted separately with phenylisocyanate and phenylisothiocyanate, followed by ring closure in an alkaline medium giving 3-[(benzimidazole-2-yl thio) methyl]-4-phenyl-1,2,4-triazole-5-ol and 3-[(benzimidazole-2-yl thio) methyl]-4-phenyl-1,2,4-triazole-5-thiol respectively (6,7). Reaction of acetohydrazide (2) with CS2 and ethanol/KOH, gave dithiocarbazate salt (8). Cyclization of (8) with hydrazine hydrate gave 3-[(benzimi
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