期刊文献+

罗氟司特新合成工艺的研究 被引量:1

Studies on Process of Synthesizing Roflumilast
下载PDF
导出
摘要 目的优化罗氟司特的合成工艺。方法以3,4-二羟基苯甲醛为起始原料,经Boc酸酐保护、醚化、脱保护、二氟一氯甲烷醚化、氧化、酰胺化反应得到目标物罗氟司特。结果与结论目标化合物的结构经MS、1H-NMR等确证。该方法原料易得,反应条件温和,危险性小,后处理简单,收率较高,有利于工业放大生产,总收率为36.3%。 OBJECTIVE To optimize the synthetic procedure of Roflumilast. METHODS Roflumilast was synthesized from 3,4-dihydroxybenzaldehyde by the reactions of Boc anhydrides protection,etherification,deprotection,monochlorodifluoromethane etherification,oxidation,amidation. RESULTS and CONCLUSION The structure of roflumilast was confirmed by MS and 1H-NMR. The synthesized route was rewarded for virtue of easy access of materials,kindness of reaction conditions,low dangerness,easy reprocessing,and good yield of 36. 3%,which are the advantages for industry.
出处 《海峡药学》 2016年第3期231-232,共2页 Strait Pharmaceutical Journal
关键词 3 4-二羟基苯甲醛 醚化 罗氟司特 3 4-Dihydroxybenzaldehyde Etherification Roflumilast
  • 相关文献

参考文献7

二级参考文献42

  • 1World Health Organization. World health statistics 2008[S].Geneva,Switzerland : World Health Organization, 2008. 被引量:1
  • 2Barnes PJ. Future treatments for chronic obstructive pulmonary disease and its comorbidities[J]. Proc Am Thorac Soc,2008,5(8) :857-864. 被引量:1
  • 3Giembycz MA,Field SK. Roflumilast: first phosphodiesterase 4 inhibitor approved for treatment of COPD[J]. Drug Des Devel Ther, 2010,21 (4) : 147-158. 被引量:1
  • 4Hatzelmann A, Morcillo EJ, Lungarella G, et al. The preclinical pharmacology of roflumilast-a selective,oral phosphodiesterase 4 inhibitor in development for chronic obstructive pulmonary disease[J]. Pulm Pharmacol Ther,2010,23(4) :235-256. 被引量:1
  • 5Hardaker EL,Freeman MS,Dale N, et al. Exposing rodents to a combination of tobacco smoke and lipopolysaccharide results in an exaggerated inflammatory response in the lung[J]. Br J Pharmacol,2010,160(8) : 1985-1996. 被引量:1
  • 6Le Quement C,Guenon I,Gillon JY,et al. The selective MMP- 12 inhibitor, ASl11793 reduces airway inflammation in mice exposed to cigarette smoke[J]. Br J Pharmacol, 2008,154 (6) 1206-1215. 被引量:1
  • 7Martorana PA,Beume R, Lueattelli M, et al. Roflumilast fully prevents emphysema in mice chronically exposed to cigarette smoke[J]. Am J Respir Crit Care Meal,2005,172(7):848-853. 被引量:1
  • 8Cortijo J, Iranzo A, Milara X, et al. Roflumilast, a phosphodiesterase 4 inhibitor, alleviates bleomycin induced lung injury[J]. Br J Pharmacol,2009,156(3) :534- 544. 被引量:1
  • 9Grootendorst DC,Gauw SA,Verhoosel RM,et al. Reduction in sputum neutrophil and eosinophil numbers by the PDE4 inhibitor roflumilast in patients with COPD[J]. Thorax,2007, 62(12) :1081-1087. 被引量:1
  • 10Hohlfeld JM, Schoenfeld Roflumilast attenuates K, Lavae-Mokhtari M, et al. pulmonary inflammation upon segmental endotoxin challenge in healthy subjects: a randomized placebo-controlled trial[J]. Pulm Pharmacol Ther, 2008,21(4) :616- 623. 被引量:1

共引文献29

同被引文献3

引证文献1

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