环丙西泮

化合物

环丙西泮(英语:Cyprazepam[1])是一种镇静催眠苯二氮䓬衍生物药物。[2][3][4][5]它具有抗焦虑特性,[6]并且可能还具有催眠骨骼肌松弛抗惊厥英语Anticonvulsant遗忘特性英语Drug-induced amnesia

环丙西泮
临床资料
给药途径口服
ATC码
  • 未分配
法律规范状态
法律规范
  • 未列入管制
药物动力学数据
药物代谢Hepatic
排泄途径Renal
识别信息
  • 10-chloro-N-(cyclopropylmethyl)-3-hydroxy-2-phenyl-3,6-diazabicyclo[5.4.0]undeca-1,6,8,10-tetraen-5-imine
CAS号15687-07-7  checkY
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
化学信息
化学式C19H18ClN3O
摩尔质量339.82 g·mol−1
3D模型(JSmol英语JSmol
  • ClC1=CC2=C(N/C(C[N+]([O-])=C2C3=CC=CC=C3)=N/CC4CC4)C=C1
  • InChI=1S/C19H18ClN3O/c20-15-8-9-17-16(10-15)19(14-4-2-1-3-5-14)23(24)12-18(22-17)21-11-13-6-7-13/h1-5,8-10,13H,6-7,11-12H2,(H,21,22) checkY
  • Key:UKFDTMNJMKWWNK-UHFFFAOYSA-N checkY

合成

编辑

苯二氮䓬类药物中的内酰胺部分对亲核试剂具有活性,并且利用这一事实制备了许多类似物。

 
环丙西泮合成[1]

例如,将地莫西泮N-环丙基甲胺加热会形成,即次要镇静剂环丙西泮。

参见

编辑

参考资料

编辑
  1. ^ 1.0 1.1 US 3138586,Wuest HM,“2-Cycloalkylamino Derivatives of 1,4-Benzodiazipines”,发行于23 June 1964,指定于Warner-Lambert Pharmaceutical Compay ; Chem. Abstr., 61: 7,032f (1964).
  2. ^ Oelschläger H, Martienssen D, Belal F. Ring Contraction of 1,4-Benzodiazepines to 3,4-Dihydroquinazolines During Macro Scale Reduction (Example 5: Cyprazepam). Archiv der Pharmazie (Wiley Interscience). 22 September 2006, 325 (8): 503–507. ISSN 0365-6233. S2CID 96638676. doi:10.1002/ardp.19923250810. (原始内容存档于5 January 2013). 
  3. ^ EP 1466628,Matthews B, Victor S, Nigel, Swindell C,“DHA-pharmaceutical agent conjugates”,发表于13 October 2004,指定于American Regent Inc. 页面存档备份,存于互联网档案馆
  4. ^ Harmonized Tariff Schedule of the United States (2009) - Supplement 1 - PHARMACEUTICAL APPENDIX TO THE HARMONIZED TARIFF SCHEDULE (PDF). USA: United States International Trade Commission. 2009 [19 September 2009]. (原始内容 (PDF)存档于31 July 2009). 
  5. ^ Schafer EW, Bowles WA, Hurlbut J. The acute oral toxicity, repellency, and hazard potential of 998 chemicals to one or more species of wild and domestic birds. Archives of Environmental Contamination and Toxicology. May 1983, 12 (3): 355–82. Bibcode:1983ArECT..12..355S. PMID 6882015. S2CID 32956594. doi:10.1007/BF01059413. 
  6. ^ World Health Organization. The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances (PDF). USA: Ministry of health, Syria. 2006 [19 September 2009].  [失效链接]