头孢地嗪酸的合成.pdfVIP

23 2 () V ol. 23 N o. 2 2009 4 JOURNA L O F UN IVERS ITY OF J INAN ( Sci. T ech) A p r. 2009 167 1- 3559 ( 2009) 02 - 0 17 6- 03 头孢地嗪酸的合成 高国庆, 郑庚修, 张淑芳 ( , 250022) 以氨噻肟酸和二乙氧基硫代磷酰氯为原料, 在碱性条件下, 制得新活性酯二乙氧基硫代磷酰- ( Z) - ( 2 - 氨基噻 唑- 4 - 基) 甲氧 氨基乙酸酯溶液( DPS 溶液) ; 与 7 - 氨基- 3- ( 5 - 羧甲基 - 4 - 甲基- 1, 3 - 噻唑- 2 - 巯甲基) 头孢- 2 - 烯 - 2 - 羧酸( TACS) 直接反应, 合成头孢地嗪酸, 以 TA CS 计产品收率达 69. 2% ( HPLC 检测, 纯度大于 99. 0% ) 头孢地嗪酸; 新活性酯; 合成 R 914. 5 A Syn thesis of C efodizim e A cid GAO G uo - q ni g, ZHENG G eng - x iu, Z HANG S hu- fa ng ( School of Chem istry and Ch em ical E ngineering, U n iv ersity of Jinan, Jinan 250022, C hina) A bstrac t: 2 - ( 2 - Am inothiazo le - 4 - y l) - 2 - m ethoxy mi inoacetic ac id reacted w ith d iethy lthiophospho ry l ch lo ride in the pres ence o f a b ase to form diethy lth iophosphory l - ( Z ) - ( 2 - am ino th iazo le - 4 - y l) - syn - m ethoxy mi inoaceta te solution ( DPS so lu tion) . Cefodizmi e ac id w as prepared by the one- step synthesis from 7 - am ino- 3- ( 5 - ( carboxym e thy l- 4 - m ethy l- 1, 3 - th ia zoly l- 2 - y l- thiom ethy l) - ceph - 3- em - 4 - carbox ylic acid ( TACS) and the D PS so lution. The y ie ld of cefodizmi e ac id reached in 69. 2% ( m on itored by HPLC, purity 99. 0% ) . K ey w ord s: ce fod iz mi e ac id; new ac tiv ity ester; synthes is , 1990 7 , , 1994 [ 1 - 3 ] [ 7- 9] ( 6R, 7R) - 7- [ ( 2 - - 4 - ) -