含硝基噁二唑啉类化合物的合成与抗菌活性
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摘要
4-硝基苯甲酸经酯化和肼解制得4-硝基苯甲酰肼,再与芳香醛反应得酰腙,最后在乙酸酐存在下发生脱水环化反应,合成了5个3-N-乙酰基-2-芳基-5-(4-硝基苯基)-1,3,4-噁二唑啉类化合物,产率为17.21%-70.15%,通过1H NMR、FT-IR对其结构进行表征,研究它们的抑菌活性,结果表明:5个化合物表现出较好的抑菌效果.
4-Nitrobenzene chlorobenzoyl hydrazine has been prepared by using desertification and hydrazinolysis of 4-nitrobenzoic acid.And then,reacting with Aryl aldehyde to give hydrazine,Last,hydrazine was reduced to 3-N-acetyl-2-aryl-5-(4-nitrophenyl)-1,3,4-oxad iazolines by ring-closing reaction in the presence of acetic anhydride and heating,yield : 17.21%-70.15%.The structures of these compounds were confirmed by 1H NMR,FT-IR.After studying their antibacterial activity,the preliminary antibacterial tests showed that all of them had good anti-bacterial activities.
4-Nitrobenzene chlorobenzoyl hydrazine has been prepared by using desertification and hydrazinolysis of 4-nitrobenzoic acid.And then,reacting with Aryl aldehyde to give hydrazine,Last,hydrazine was reduced to 3-N-acetyl-2-aryl-5-(4-nitrophenyl)-1,3,4-oxad iazolines by ring-closing reaction in the presence of acetic anhydride and heating,yield : 17.21%-70.15%.The structures of these compounds were confirmed by 1H NMR,FT-IR.After studying their antibacterial activity,the preliminary antibacterial tests showed that all of them had good anti-bacterial activities.
引文
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[4]SHAOYONG KE,LIU FENGYLI,WANG NI,etal.1,3,4-Ox-adiazoline derivatives as novel potential inhibitors tar-getting chitinbiosynthesis:Design,synthesis and biology-cal evaluation[J].Bioorganic&Medicinal Chemistry Letters,2009,19:332-335.
[5]李德江,黄明权,葛正红.3-N-乙酰基-2-芳基-5-(4-硝基苯基)-1,3,4,-噁唑啉类化合物的合成与结构表征[J].精细化工,2005,22(4):283-286.
[6]张友胜,宁正祥,杨伟丽.藤茶学[M].广州:广东科技出版社,2003:79-88.
[2]KHANUM SHAUKATH ARA,SHASHIKANTH S S.Microwave-as-sisted synthesis of2-amino and2-azetidinonyl 5-(2-benzoyl-phenoxymethyl)-1,3,4-oxadiazoles[J].Heteroatom Chemistry,2004,15(1):37-42.
[3]MICHAEL AHEARN,POET-YOON CHANYAPUTHIPONG.Preparation and spectroscopic of3-acyl-1,3,4-oxadiazolines[J].Heterocyclic Chem.,1995,32:1647-1649.
[4]SHAOYONG KE,LIU FENGYLI,WANG NI,etal.1,3,4-Ox-adiazoline derivatives as novel potential inhibitors tar-getting chitinbiosynthesis:Design,synthesis and biology-cal evaluation[J].Bioorganic&Medicinal Chemistry Letters,2009,19:332-335.
[5]李德江,黄明权,葛正红.3-N-乙酰基-2-芳基-5-(4-硝基苯基)-1,3,4,-噁唑啉类化合物的合成与结构表征[J].精细化工,2005,22(4):283-286.
[6]张友胜,宁正祥,杨伟丽.藤茶学[M].广州:广东科技出版社,2003:79-88.