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|a The work presented in the current thesis is concerned with the synthesis of some new 1,2,4-triazole and 1,3 –oxazepine-4,7-dione derivatives using the microwave method and according to the following parts; Part one:- Synthesis of 1,3-oxazepine-4,7-dione with aliphatic hydrocarbon. 1-Conversion of the appropriate aliphatic and aromatic esters to their corresponding hydrazides by reaction with hydrazine hydrates [N1- N4]. 2- Conversion of the benzoic acid directly to the benzoyl hydrazine [N5]. 3- Conversion of the hydrazides of aliphatic carboxylic acid to their corresponding hydrazones through condensation process between hydrazides and appropriate aromatic aldehydes in the presence DMF as solvent[N6-N36]. 4-Cycloaddition reaction of hydrazones with maleic and phthalic anhydrides afforded 1,3-oxazepine-4,7-dione derivatives [N88-N140],respectively. Part two:- Synthesis of 1,3-oxazepine-4,7-dione with 1,2,4-triazole 1- Conversion of the hydrazides to the[ dipotassium salt-2,2`-(dioxoalkane-diyl)dihydrazinecarbodithioate] through the reaction between these hydrazides and CS2 in the presence of KOH as base , [N37-N40]. 2-Preparation of 4-amino-1,2,4-triazole derivatives through the reaction of potassium salts with hydrazine hydrate using refluxing method[N41-N43].
|a 3- Conversion of the triazole derivatives to the Schiff`s bases, through the condensation process between triazoles and benzaldehyde derivatives [N44-N76]. 4- Cycloaddition reaction of these triazole containing Schiff base [N44-N76] with maleic and phthalic anhydrides afforded 1,3-oxazepine-4,7-dione derivatives [N141-N195]. Part three:- Synthesis of 1,3-oxazepine-4,7-dione containing sulfonamide moiety. 1-Preparation of Schiff`s base derivatives of p-aminosulfonamide through the condensation process with benzaldehyde derivatives [ N77-N87]. 2-Cycloaddition reaction between Schiff`s base of p-aminosulfonamide derivatives with maleic and phthalic anhydrides ,afforded 1,3-oxazepine-4,7-dione derivatives [N196-N217]. 3-preparation of bis-Schiff`s base of p-amionsulfonamide through the condensation process between p-amionsulfonamide and two mole of benzaldehyde derivatives [ N218-N220]. 4-cyclic addition reaction between bis-Schiff`s base of p-aminosulfonamide derivatives with maleic and phthalic anhydrides ,afforded 1,3 –oxazepine -4,7-dione derivatives [N221-N226]. The structure of the prepared compounds were established using available spectroscopic methods (IR , 1HNMR , 13CNMR, CHN )and also observing the change in physical states of the starting material such as (colour and melting point) and the results Obtained from these methods gave us good indication to the proposed structures. The biological activity evaluation for some synthesized compound ( N204,N198,N211,N213,N199,N214,N85,N215,N206,N196,N197 ) were also studies against five type of bacteria(Staphylococciaurues, Escherichia coli,Kelbesillapneumonia, Pseudomonasaeruainosa, Streptococuspyogene) and the result obtained The more stable configurationally structures for 1, 3-oaxzepine ring were examined using ChemiOffice( 2004)
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