全部 标题 作者
关键词 摘要

OALib Journal期刊
ISSN: 2333-9721
费用:99美元

查看量下载量

相关文章

更多...
同位素  2014 

吉西他滨-13C,15N2及其代谢产物的合成

DOI: 10.7538/tws.2014.27.02.0082, PP. 82-86

Keywords: 同位素标记,合成,吉西他滨-13C,15N2,吉西他滨代谢物-13C,15N2

Full-Text   Cite this paper   Add to My Lib

Abstract:

以自制的尿素-13C,15N2为前体,与3-乙氧基丙烯腈反应制备胞嘧啶-13C,15N2,用BSA保护后,经与2-脱氧-2,2-二氟-D-赤式-五呋喃糖-3,5-二苯甲酯-1-甲磺酸酯反应生成2',2'-二氟-2'-脱氧胞嘧啶核苷-3',5'-二苯甲酸酯-13C,15N2,分离纯化后经NaOH水解生成吉西他滨-13C,15N2,再进一步降解脱氨得到吉西他滨-13C,15N2代谢产物。产品经HPLC,LC-MS和1HNMR表征确定,化学纯度高于98%,13C同位素丰度为99%,15N同位素丰度为98%。结果表明,合成的吉西他滨-13C,15N可用于药物代谢研究。

References

[1]  霍伟,曲范杰,范丽听. 吉西他滨联合卡铂线治疗晚期非小细胞肺癌疗效观察[J]. 临床肿瘤学杂志, 2006, 11(11): 828-829.Huo Wei,Qu Fanfie,Fan Lixin. Efects of gemcitabine plus carboplatin in threatment of chem onaive patients with advanced non-small cell lung cancer[J]. Chinese Clinical Oncology, 2006, 11(11):828-829(in Chinese).
[2]  Paul A, Bunn J. Triplet chemotherapy with gemcitabine, a platinum and a third agent in the treatment of advanced non-small-cell lung cancer[J]. Semin Oncol, 1999, 26(1): 25-30.
[3]  Hertel LW, Kroin JS. Synthesis of 2-deoxy-2,2-difluoro-D-ribose and 2-deoxy-2,2'-difluoro-D-ribofuranosyl nucleosides [J]. J Org Chem, 1988, 53 (11) : 2406-2409.
[4]  Chou TaSen, Heath PC. Process for and intermediates of 2’-2’-difluoronucleosides:USA patent,US5223608[P]. 1990-07-12.
[5]  顾海成,马玉恒,王伟. 盐酸吉西他滨的合成方法:中国,102417533A[P]. 2011-10-28.
[6]  李高. 稳定同位素标记药物在临床药代动力学研究中的应用[J]. 中国临床药理学杂志, 2000, 1(16): 58-62.LI Gao. The Application of Stable Isotope Labelled Drugs in Clinical Pharmacokinetic Study[J]. The Chinese Journal of Clinical Pharmacology, 2000, 1(16): 58-62(in Chinese).
[7]  Victor C. Nelson. Synthesis of isotopically labelled DNA degradation products for use in mass spectrometric studies of cellular DNA damage[J]. Journal of Labelled Compounds and Radiopharmaceuticals, 1996, 38(8): 713-723 ;
[8]  蔡东,商琳琳,贾云宏,等. 胞嘧啶的合成研究进展[J]. 化工中间体, 2009, 2: 14-17; Cai Dong, Shang Linlin, Jia Yunhong, etc. Progress in the synthesis of cytosine[J]. Chemical Intermediates, 2009, 2: 14-17(in Chinese);
[9]  霍利春,李春新,刘茵. 胞嘧啶合成新工艺[J]. 甘肃石油和化工, 2012, 2:28-32. Huo Lichun, Li Chunxin, Liu Yin. New technology of synthesis Cytosine[J]. gansu shiyou he huagong, 2012, 2:28-32(in Chinese).

Full-Text

Contact Us

service@oalib.com

QQ:3279437679

WhatsApp +8615387084133