|
|
|
| Synthetic Technology Process of Penicillin sulfoxide |
| YAN Feng1,ZHANG Gui-hua2 |
| 1.NCPC Hebei Huamin Pharmaceutical Corporation Ltd., Shijiazhuang 052165, China; 2.Beijing Kerui Boyuan Technology Corporation Ltd., Beijing 100083, China |
|
|
|
|
Abstract 7-Amino-3-desacetoxy cephalosporanic acid ( 7-ADCA ) is an important intermediate of cephalosporin antibiotics parent, which is prepared via ring-expanding and dissociation of penicillin sulfoxide. The production process of penicillin sulfoxide which is the important intermediate of 7-ADCA and its synthetic technology progress at home and abroad were summarized. That the optimized direction of the penicillin sulfoxide synthesis process was given. It is pointed out that crystallization step of the crude product still needs to be simplified and optimized because the increase of the yield is refrained by the emissions of all kinds of crystal mother solution in different technical process and the environment is also damaged.
|
|
|
|
|
|
| [ 1 ] 中国科学院化工冶金研究所. 脱除青霉素G亚砜粗产品中水分及杂质的方法:中国,CN 00109866[ P ]. 2000.
[ 2 ] 冯胜昔,刘晓红,黄敏康,等.青霉素氧化产物的鉴别及其转化方法[ J ]. 中国抗生素杂志,1999,24(3 ):178-179.
[ 3 ] 华北制药集团有限责任公司. 一种青霉素G亚砜复合晶体及其制备方法:中国,CN 200810054515[ P ]. 2008.
[ 4 ] 华北制药河北华民药业有限责任公司. 一种青霉素G亚砜DMF复合晶体及其制备方法:中国,CN 201210557522[ P ]. 2012.
[ 5 ] 华北制药河北华民药业有限责任公司. 一种青霉素G亚砜DMA复合晶体及其制备方法:中国,CN 201210557723[ P ]. 2012.
[ 6 ] 张存瑜.青霉素氧化的工艺改进[ J ]. 中国医药工业杂志,1995,26(11 ):483-484.
[ 7 ] 张方丽. 头孢菌素类抗生素中间体7-ADCA合成工艺研究[ D ]. 天津:天津大学,2003.
[ 8 ] 张立杰,李 巍,刘东志,等. 青霉素G钾催化氧化制备青霉素G亚砜的研究[ J ]. 中国抗生素杂志,2003,28(7 ):391-393.
[ 9 ] Palomo Coll. Alberto ( Gema S.A ) Oxidation of sulfide Groups in Penicillin derivatives:Span,ES 509855[ P ]. 1983-02-01.
[10] 史兰香,赵地顺,徐志栋,等. 青霉素亚砜的制备[ J ]. 河北工业科技,1998,15(2 ):40-42.
[11] Hideo Tanaka, Tyo Kikuchi, Sigeru Torii.Chemoselective Aerobic Oxidation of Penicillin and Cephalosporin Derivatives into Sulfoxides[ J ].Tetrahedron,1996, 52(7 ):2 343-2 348.
[12] D O Spry.Oxidation of Penicillin and Dihydrocephalosporin Deriva-tives with Ozone [ J ]. J Org Chem,1972,37( 5 ):793-795.
[13] 刘东志,曲红梅,肖 义,等. 7-氨基去乙酰氧基头孢烷酸(7-ADCA )的合成研究I.青霉素G钾盐的氧化[ J ]. 中国抗生素杂志,2000,25(2 ):103-104.
[14] 史兰香,陈焕章,赵地顺,等.青霉素制备青霉素亚砜的研究[ J ]. 精细化工,2000,17(5 ):252-276.
[15] 袁辉环,魏 巍,田 蕾,等.青霉素V亚砜酸的制备[ J ]. 长春工业大学学报,2007,28(1 ):14-16.
[16] 杨 莉,刘智凌. 青霉素G亚砜的合成[ J ]. 精细化工中间体,2007,37(6 ):36-38.
[17] 苗 勇,亓平言,苏玉山.青霉素萃取工艺条件研究[ J ]. 清华大学学报(自然科学版),1999,39(10 ):77-80.
[18] 浙江昂利康制药有限公司. 一种头孢类中间体青霉素亚砜的制备:中国,CN 201310459281[ P ]. 2013.
[19] 天津大学. 一种制备青霉素亚砜的方法:中国,CN 201010502975[ P ]. 2010. |
|
|
|