期刊文献+
任意字段
题名或关键词
题名
关键词
文摘
作者
第一作者
机构
刊名
分类号
参考文献
作者简介
基金资助
栏目信息

罗氟司特的合成方法研究进展 被引量：3

Progress in Synthetic Methods of Roflumilast
原文传递
导出
摘要 罗氟司特是一种第二代磷酸二酯酶4抑制剂,是首个用于治疗慢性阻塞性肺病的新型药物,具有药效高、服用安全等优点和广阔的市场前景。本文综述了近年来国内外报道的罗氟司特的合成方法研究进展,并讨论了各方法的优缺点以期对其工业化生产提供依据。 Roflumilast is one of the second generation PDE-4 inhibitors and the first drug for the treatment of chronic obstructive pulmonary disease. It has displayed high efficacy and a good safety profile and has broad market prospect. Research progress in its synthetic methods reported at home and abroad was reviewed and the advantages and disadvantages of each method were discussed.
作者 林艳 刘帅 陈立功 房桂干
机构地区 中国林业科学研究院林产化学工业研究所 中国林业科学研究院制浆造纸研究开发中心 天津大学化工学院 浙江兴欣化工有限公司
出处 《化学通报》 CAS CSCD 北大核心 2014年第4期319-323,共5页 Chemistry
基金 中央级公益性科研院所专项基金项目(CAFINT2011K02)资助
关键词 罗氟司特 慢性阻塞性肺病 合成方法 Roflumilast Chronic obstructive pulmonary diseases Synthetic method
分类号 TQ463-1 [化学工程—制药化工]
  • 相关文献

参考文献2

二级参考文献28

  • 1贺蓓.多中心随机对照临床研究表明Roflumilast可以改善慢性阻塞性肺病患者的肺功能[J].中华医学杂志,2005,85(36):2546-2546. 被引量：1
  • 2RABE KF. Roflumilast for the treatment of chronic obstructive pulmonary disease [ J ]. Expert Rev Respir Med, 2010, 4 ( 5 ) : 543 -555.
  • 3RABE KF, HURD S, ANZUETO A, et al. Global strategy for the diagnosis, management, and prevention of chronic obstructive pulmonary disease: GOLD executive summary [ J ]. Am Respir Crit Care Med, 2007,176 ( 6 ) : 532 - 555.
  • 4MANNINO DM, HOMA DM, AKINBAMI LJ, et al. Chronic ob- structive pulmonary disease surveillance: United States, 1971 - 2000[J]. MMWR CDC Surveill Summ, 2002, 51 (6) :1 - 16.
  • 5HATZELMANN A, MORCILLO EJ, LUNGARELLA G, et al. The preclinical pharmacology of roflumilast: a selective, oral phosphodiesterase inhibitor in development for chronic obstructive pulmonary disease[ J ]. Pulm Pharmacol Ther, 2010, 23 (4) : 235 -256.
  • 6PRESS NJ, BANNER KH. PDE4 inhibitors-a review of the current field[ J]. Prog Med Chem, 2009, 47 (1) :37 -74.
  • 7WOHLSEN A, HIRRLE A, TENOR H, et al. Effect of cyclic AMP elevating agents on airway ciliary beat frequency in central and lateral airways in rat precision-cut lung slices [ J ]. Eur J Pharmacol, 2010, 635 ( 1 - 3 ) : 177 - 183.
  • 8CHAPMAN RW, HOUSE A, JONES H, et al. Effect of inhaled roflumilast on the prevention and resolution of allergen-induced late phase airflow obstruction in Brown Norway rats [ J ]. Eur J Pharmacol, 2007, 571 (2 - 3) :215 -221.
  • 9HOHLFELD JM, SCHOENFELD K, LAVAE-MOKHTARI M, et al. Roflumilast attenuates pulmonary inflammation upon segmen- tal endotoxin challenge in healthy subjects: a randomized place- bocontrolled trial [ J ]. PulmPharmacol Ther, 2008, 21 ( 4 ) : 616 - 625.
  • 10Roflumilast[ EB/OL]. [ 2011 - 04 - 12 ]. http ://www. accessda- ta. fda. gov/scripts/cder/drugsatfda/ind ex. cfm? fuseaction = Search. Label_ApprovalHistory.

共引文献21

同被引文献16

  • 1Rabe K F. Roflumilast for the treatment of chronic obstructive pulmonary disease [J]. Expert Rev Respir Med, 2010, 4 (5): 543-555.
  • 2Poole P, Black P N, Cates C J. Mucolytic agents for chronic bronchitis or chronicobstructive pulmonary disease [J]. Cochrane Database Syst Rev, 2012, 8: CD001287.
  • 3Reid D J, Pham N T. Emerging therapeutic options for the management of COPD [J]. Clin Med lnsights Circ Respir Pulm Med, 2013, 7: 7-15.
  • 4Tashkin D P, Varghese S T. Combined treatment with formoterol and tiotropium is more efficacious than treatment with tiotropium alone in patients with chronic obstructive pulmonary disease, regardless of smoking status, inhaled corticosteroid use, baseline severity, or gender [J]. Pulm Pharmacol Th er, 2011, 24(1): 147 - 152.
  • 5Cook D C, Jones R H, Kabir H, et al. Process development of the PDE IV inhibitor 3-(cyclopentyloxy)- N-(3,5-dichloropyrid-4-yl)-4-methoxybenzamide [J]. Org Proc Res Dev, 1998, 2(3): 157-168.
  • 6Zhou Y, Wang X, Zeng X, et al. Positive benefits of theophylline in a randomized, double-blind, parallel- group, placebo-controlled study of low-dose, slow-release theophylline in the treatment of COPD for 1 year [J]. Respirology, 2006, 11(5): 603-610.
  • 7Lin Y, Huang P J, Liu S, et al. A convenient method for the synthesis of roflumilast [J]. Res Chem Intermediat, 2013, 39(5): 2107-2113.
  • 8Williams L E,Wu T C.Process for production of fluoroalkoxy-substituted benzamides(roflumilast and intermediates):US,6822114B1[P].2004-11-23.
  • 9Bose P,Sachdeva Y P,Rathore R S,et al.Process for the preparation of roflumilast:US,7470791B2[P].2008-12-30.
  • 10Yan L,Pei J H,Shuai L,et al.A convenient method for the synthesis of roflumilast[J].Res Chem Intermed,2013,39(5):2107-2113.

引证文献3

二级引证文献3

化学通报
2014年 第4期

相关作者

内容加载中请稍等...

相关机构

内容加载中请稍等...

相关主题

内容加载中请稍等...

浏览历史

内容加载中请稍等...
;
使用帮助 返回顶部