Apalutamide合成路线图解
详细信息    查看全文 | 推荐本文 |
  • 英文篇名:Graphical Synthetic Routes of Apalutamide
  • 作者:王希 ; 刘水平
  • 英文作者:WANG Xi;LIU Shui-ping;Zhuzhou Institute for Food and Drug Control;
  • 关键词:Apalutamide ; 合成路线图解
  • 英文关键词:Apalutamide;;Graphical Synthetic Routes
  • 中文刊名:HAIX
  • 英文刊名:Strait Pharmaceutical Journal
  • 机构:湖南省株洲市食品药品检验所;
  • 出版日期:2019-04-15
  • 出版单位:海峡药学
  • 年:2019
  • 期:v.31;No.231
  • 语种:中文;
  • 页:HAIX201904017
  • 页数:3
  • CN:04
  • ISSN:35-1173/R
  • 分类号:55-57
摘要
目的通过对已有的Apalutamide的合成方法进行分析,从而找到最适宜工业化生产的路线。方法对Apalutamide的合成路线进行概括、归纳。结果与结论路线3原料价廉易的,反应路线短,更加符合工业生产要求。
        OBJECTIVE To review the existing synthetic routes,and find the most ideal synthetic routes of Apalutamide for industrialization.METHODS The different synthetic processes of Apalutamide were generalized.RESULTS and CONCLUSION The route 3 with the starting material ornithine shows more favorable and commercial value in the manufacturing scale.
引文
[1]Janseen.ERLEADA (apalutamide),a next-generation androgen receptor inhibitor,granted U.S.FDA approval for the treatment of patients with non-metastatic castration-resistant prostate cancer[EB/OL].(2018-02-14)[2018-02-25].http://www.janssen.com/erleada-apalutamidenext-generation-androgen-receptor-inhibitor-granted-us-fda-approvaltreatment.
    [2]Rathkopf D E,Smith M R,Ryan C J,et al.Androgen receptor mutations in patients with castration-resistant prostate cancer treated with apalutamide[J].Ann Oncol,2017,28(9):2264-2271.
    [3]Rathkopf DE,Morris MJ,Fox JJ,et al.Phase Ⅰ study of ARN-509,a novel antiandrogen,in the treatment of castration-resistant prostate cancer[J].J Clin Oncol,2013,31(28):3525-3530.
    [4]Jung ME,Ouk S,Yoo DW,et al.Structure-activity relationship for thiohydantoin androgen receptor antagonists for castration-resistant prostate cancer(CRPC)[J].J Med Chem,2010,53(7):2779-2796.
    [5]Clegg NJ,Wongvipat J,Joseph JD,et al.ARN-509:A novel antiandrogen for prostate cancer treatment[J].Cancer Res,2012,72(6):1494-1503.
    [6]Jung ME,SAWYERS CL,Ouk S,et al.Androgen receptor modulator for the treatment of prostate cancer and androgen receptor associated diseases:WO,2007,126765[P].2007-11-08.
    [7]Ouerfelli O,Dilhas A,Yang G,et al.Synthesis of thiohydantoins:WO,2008119015[P].2008-10-02.
    [8]魏德康,平晓晴,彭嘉娟,赵伟伟,朱雪焱.阿帕鲁胺的合成工艺改进[J].中国医药工业杂志,2018(04):440-444.

© 2004-2018 中国地质图书馆版权所有 京ICP备05064691号 京公网安备11010802017129号

地址:北京市海淀区学院路29号 邮编:100083

电话:办公室:(+86 10)66554848;文献借阅、咨询服务、科技查新:66554700