New Schiff bases derivatives [IV]a-e is prepared via condensation of Derythroascorbic acid with p-substituted aldehydes in dry benzene. To obtain these derivatives, the 5,6-O-isopropylidene-L-ascorbic acid[I] was chosen as starting material, compound prepared from the reaction of L-ascorbic acid as starting material. Compound[I] was prepared from the reaction of L-ascorbic acid with dry acetone in the presence of hydrogen chloride. The esterification of hydroxyl groups at C-2 and C-3 positions with excess ofethyl α –chloroacetate in the presence of sodium acetate produce acorresebonding ester [II] , which was condensed with hydrazine hydrate to give new hydrazide [III] . The new Schiff bases [IV]a-e were synthesized by reaction of acid hydrizide with different p-substituted benzaldehyde in dry benzene . The new 1,3- oxazepine derivatives [V]a-ewere obtained by Diels-Alder reaction of Schiff bases with phthalic anhydride in dry benzene (Scheme 1) . All the synthesized compounds have been characterized by melting points , FTIR and 1HMNR (of some of theme) spectroscopy. The biological activity of synthesized compounds was examined against two types of bacteria; G(+) and G(-).
In this study, new derivatives of 3-C-spiro ring nucleoside analogues were synthesized. The structures of these derivatives were characterized by infrared spectroscopy,1HNMR (some of them) and elemental analysis. The nucleoside derivatives were tested for inhibition of E-coli and were all found to be active.
Solvent- free thermal heating, one-pot condensation of acetophenone, ethyl cyanoacetate or malononitrle and substituted Aromatic aldehyde, ammonium acetate give, 2oxo-3-cyano-4-substituted Aryl-6-phenyl pyridine [I]a-h , or 2-amino-3-cyano-4-substituted Aryl-6-phenyl pyridine derivatives[II]a-f , respectively. Treatment of compounds 2-oxo-3-cyano-4-substituted Aryl-6-phenyl pyridine with phosphorous penta sulphide (P2S5), give 2-thioxo-3-cyano-4-substituted Aryl-6-phenyl pyridine derivatives[III]a-c . All prepared compounds
... Show MoreNew Fourteen compounds were synthesized in four steps. The first step included synthesis of 2-biphenyl fused ring of imidazo(1,2- a)pyrimidine from the reaction of 2-aminopyrimidine and biphenyl phenacyl bromide . The second step was introduced aldehyde group from the reaction of 2-biphenyl fused rings of imidazo(1,2-a)pyrimidine with POCl3 in presence of DMF and CHCl3. 3-Carbaladehyde derivatives of fused imidazo/pyrimidine was reacted with different aromatic amines to afford new Schiff bases. These new 3- imines derivatives was reduced by using sodiumborohydride to yield another new 3-aminomethyl-2-biphenyl imidazo (1,2-a)pyrimidine derivatives in moderate yield .Some new prepared compounds were identified by melting point, FT- IR , 13C-
... Show MoreIn this research, a new 1, 3, 4-Thiadiazole derivatives have been synthesized by many heterocyclic reactions. Starting from (2, 5 – dimercapto -1, 3, 4-Thiadiazole) a variety of derivatives have been synthesis. Compound (1) was synthesized by the reaction of hydrazine hydrate with carbon disulphide in absolute ethanol. The compound (1) was reacted with 1, 2-dibromoethane in presence of alkali ethanol to give the compound (2). The compound (3) was formed from the reaction of compound (2) with hydrazine hydrate. Schiff base (4) was obtained by reacting of compound (3) with the compound (p-hydroxybenzaldehyde) in absolute ethanol. A variety of phenolic Schiff base (Methylolic, Etheric, and Epoxy) derivatives have been synthesized. Methylol
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(1)
A series of new 1,8-naphthalimides linked to azetidinone, thiazolidinone or tetrazole moieties were synthesized. N-ester-1,8-naphthalimide (1) was obtained by direct imidation of 1,8-naphthalic anhydride with ethylglycinate. Compound (1) was treated with hydrazine hydrate in absolute ethanol to give N-acetohydrazide-1,8-naphthalimide (2). The hydrazine derivative (2) was used to obtain new Schiff bases (3-7). Three routes with different reagents were used for the cyclization of the prepared Schiff bases. Fifteen cyclic Schiff bases (8-22) with four- and five-membered rings were obtained.
The structures of the newly synthesized compounds were identified by their FTIR, 1H-NMR, 13C-NMR spectral data and some physical properties. Furtherm
A series of new 2-quinolone derivatives linked to benzene sulphonyl moieties were performed by many steps: the first step involved preparation of different coumarins (A1,A2) by condensation of different substituted phenols with ethyl acetoacetate. The compound A1 was treated with nitric acid to afford two isomers of nitrocoumarin derivatives (A3) and (A4). The prepared compounds (A2, A3) were treated with hydrazine hydrate to synthesize different 2-quinolone compounds (A5,A6) while the coumarin treated with different amines gave compounds (A7,A8). Then the synthesized 2-quinolone compounds (A5-A8) treated with benzene sulphonyl chloride to afford new sulfonamide derivatives (A9-A12). The synthesized compounds were characterized by FT-IR, 1H
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Stable new derivative of L-ascorbic acid, 5,6-O-iso propylidene 2,3-O,O acetic acid-Lascorbic acid (L) was synthesized in good yield by the reaction of 5,6-O-isopropylidene-Lascorbic acid with chloroacetic acid in presence of potassium hydroxide. The new product (L) was characterized by 1H, 13C–NMR, mass spectrum and fourier transform infrared (FTIR). The reaction of the ligand (L) with metal bivalent ion., M+2 = (Co, Ni, Cu, Cd, Hg, Mg, Ca, Pb) synthesized and characterized by FTIR, UV-Visible, Molar conductance, Atomic absorption and the molar ratio (Ni+2, Cd+2) complexes. Spectroscopic evidence showed that the binding of the M(II) ions with (L) are through the (C–I=O) Lacton and O-2-CH2COO– as a bidentate manar re
... Show MoreThe work includes synthesis of 1,2,3-triazoles via click conditions and using the microwave irradiation starting from two synthesized azides: 2,3,4,6-tetra-O-acetyl-β-D-glucopyranosyl azide (5) and perfluorobutylethyl azide (10) and different terminal alkynes. It also includes microwave enhanced synthesis of tetrazoles via the reaction of two synthesized azides i.e., perfluorobutylethyl azide (10) and 1,5-diazidopentane (13) with benzoyl cyanide. Most of the prepared compounds have been characterized by: TLC, FT-IR, 1H NMR, 13C NMR, LC-MS and microelemental analysis
Schiff bases (Sh1-Sh3) have been synthesized (p-aminophenol) was condensed with different aromatic aldehyde in ethanol inthe presence of glacial acetic acid as catalyst. These Schiff bases on treatment with monochloroacetyl choride gave 3-chloro-1-(4-hydroxyphenyl)-4-(substituted)azetidin-2-one(Az4-Az6), with αmercaptoacetic acid gave 3-(4-hydroxyphenyl)-2-( substituted)thiazolidin-4-one (Th7-Th9) and with anthranilic acid gave 3-(4-hydroxyphenyl)-2(substituted)-2,3-dihydroquinazolin-4(1H)-one (Qu10-Qu12). The purity of the derivatives was confirmed by TLC. The some compoundsidentify by (FT-IR and1H, 13C-NMR) data. Some of derivatives were evaluated activity against several microbesto determine ability to inhibit bacterial in some h
... Show MoreIn vivo study was made for the coumpounds 3-(ocetyl Salicyloyl)-5,6-O-isoprpy lideneL-ascorbicocid,2,3-(acetyl Salicyloyl )-5,6-o- isopropylidene-L-ascorbic acid and 2,3,5,6(acetyl Salicyloyl )-L- ascorbic acid .And a measurement was mod for the concentration of the liberated aspirin in blood samples a fter (2,3,4,6,8,10) hours of the initial dose for the animal .The results showed that the highest concentration of aspirin was after four hours of giving the dose to the animal which is in accordance with pharmacokinetics studies