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头孢他啶侧链酸活性硫酯的合成研究
引用本文:王玉环.头孢他啶侧链酸活性硫酯的合成研究[J].石家庄职业技术学院学报,2009,21(2):33-35.
作者姓名:王玉环
作者单位:石家庄职业技术学院,化学工程系,河北,石家庄,050081
摘    要:头孢他啶侧链酸在碱性条件下与DM缩合生成头孢他啶侧链酸活性硫酯时,用价格低廉的亚磷酸三乙酯代替价格昂贵的三苯基膦,通过设计正交实验优选出的较佳反应条件为:固定头孢他啶侧链酸19.8g,反应物料n(头孢他啶侧链酸):n(DM):n(亚磷酸三乙酯):n(三乙胺)=1:1.2:1.2:1.2,反应溶剂乙腈150mL,于5℃反应5h,收率86.8%.

关 键 词:头孢他啶  侧链酸  活性硫酯  合成

Synthesis of 2-(2-amino-4-thiazolyl)-(Z) -2- [(1 -tert-butoxycarbonyl-1-methyl-ethoxy) -imino]acetic acid benzothiazolyl thioester
WANG Yu-huan.Synthesis of 2-(2-amino-4-thiazolyl)-(Z) -2- [(1 -tert-butoxycarbonyl-1-methyl-ethoxy) -imino]acetic acid benzothiazolyl thioester[J].Journal of Shijiazhuang Vocational Technology Institute,2009,21(2):33-35.
Authors:WANG Yu-huan
Institution:WANG Yu-huan (Department of Chemistry, Shijiazhuang Vocational Technology Institute, Shijiazhuang, Hebei 050081, China)
Abstract:The condensate ( Z )-2- ( 2-aminothiazol-4-yl )-2- ( tert. -butyoxycarbonylprop-2-oxyimino ) acetic acid forms 2- ( 2-amino-4-thiazolyl ) - ( Z ) -2- ( 1-tert-butoxycarbonyl-l-methyl-ethoxy ) -imino ] with DM, in alkali conditions, acetic acid benzothiazolyl thioester, by triethyl phosphate instead of the expensive triphenylphosphine. The optimum conditions were studied through the orthogonal experiment: (Z)-2-(2-aminothiazol- 4-yl)-2- ( tert. -butyoxycarbonylprop-2-oxyimino) acetic acid 19.8 g, n ( (Z)-2- (2-aminothiazol-4-yl)-2- ( tert. -butyoxycarbonylprop-2-oxyimino)aceticacid) : n(DM) :n(triethyl phosphite) : n(triethylamine) = 1 : 1.2: 1.2: 1.2, with reaction solvent acetonitrile of 150 ml;reaction temperature of 5 IE and reaction time of 5 h. The yield of product is up to 86.8 %.
Keywords:ceftazidime  side chain acid  activated thioester  synthesis
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