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To achieve this, the ester 0.5 M in methanol and hydroxyl amine 10 eq was reacted in the presence of sodium methoxide 1 eq.

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29 The wide biological application of hydroxamates necessitates the review of its synthesis and biological applications. General Synthesis of Weinreb Amides Hydroxamic acids are prepared usually from esters or acid chlorides or carboxylic acids.2.1. Protection of the commercially available hydro ester 22 with tertiary-butyldimethylsilyl chloride TBDMS-Cl gave silyl ester 23. The ester 23 on reduction with Li BH4 gave the alcohol. Carbodiimides hydrolyze to form ureas, which makes them uncommon in nature. Hydroxyurea are also used for treatment of chronic myelogenal leukemia, myeloproliferative syndromes and sickle cell anemia. 2 Hydroxamates of amino acids are effective inhibitors of amino peptidases. From the perspective of small molecule activation, carbodiimides are. Hydroxamates such as fosmidomycin and desferrioxamine B are potent antimalarial agent. Ugwuja, Synthesis and Biological Applications of Hydroxamates, American Journal of Organic Chemistry, Vol. 3 Their mode of action results from the formation of bidentate ligand with active site of zinc. Ugwu, Department of Pure and Industrial Chemistry, University of Nigeria, Nsukka, Nigeria. Abstract Hydroxamates are physiologically active compounds. They have found applications as histone deacetylase inhibitors widely applied in cancer treatment such as vorinostat, belinostat, panobinostat and trichostatin A. They are amides where the hydrogen H atom of NH center has been replaced by an OH. Hydroxamates are deprotonated product of hydroxamic acid and acts as excellent ligand.

Ugwuja3 1Department of Pure and Industrial Chemistry, University of Nigeria, Nsukka, Nigeria 2National Centre for Energy Research and Development, University of Nigeria, Nsukka, Nigeria 3Department of Chemical Sciences, Federal University, Wukari, Nigeria Correspondence to: David I. Introduction Hydroxamates are class of organic compounds bearing the functional group RICON OH RII as organic residues and CO as a carbonyl group.

Oxidation of alcohol 24 under Swern condition 47 gave aldehyde 25 which was treated with an aryl Grignard reagent to produce alcohol 26.

Alcohol 26 was treated with 2-methoxy propene and pyridinium p-toluenesulfonate PPTS to generate protected diol 27.

Synthesis of Benzohydroxamic Acid 3 The synthesis of compound 3 was achieved by reacting methyl benzoate 1 and hydroxylamine 2. Synthesis of Hydroxamates Using N, N1, NII–trimethoxy-N, NI, NII-trimethyl Phosphorus Triamides 5 Nui et al 31 reported the conversion of aromatic and aliphatic carboxylic acids, including sterically hindered substrates directly to hydroxamates using N, NI, NII-trimethoxy-N, NI, NII–trimethyl phosphorus triamide 5.

On condensation of aromatic or aliphatic carboxylic acid 4 0.01M and compound 5 0.005M in toluene at 60 for 0.5 to 1 h, the hydroxamate 6 was obtained in excellent yield. Ester Synthesis of Hydroxamate Riva et al 32 reported the transformation of methyl or ethyl carboxylic esters into the corresponding hydroxamic acid.

Keywords: Keyword Histone deacetylase inhibitors, Matrix metalloproteinase inhibitors, HIV, Hydroxamaates, Ribonucleoside diphosphate reductase Cite this paper: David I. The reasonable way of producing hydroxamic acid derivative is the reaction of hydroxylamine with acid chlorides or esters.