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消旋棉酚拆分的研究——Ⅳ.苏(-)或(+)-1-(对硝基苯基)-1,3-二羟基丙胺-2为拆分剂 被引量:2

STUDIES ON THE RESOLUTION OF RACEMIC GOSSYPOL Ⅳ. USE OF THREO (-) OR (+)-1-(p-NITROPHENYL)-1,3-DIHYDROXYPROPYLAMINE-2 AS THE RESOLVING AGENT
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摘要 本文介绍以光学活性苏-1-(对硝基苯基)-1,3-二羟基丙胺-2为拆分剂,与消旋棉酚缩合,用常压柱色谱或溶剂结晶法分离得到两个光学纯的非对映体,然后分别水解得(+)和(-)-棉酚。 Threo (-) or (+)-1-(p-nitophenyl )-1, 3-dihydroxy propylamine -2 was found to be a useful resolving agent for racemic gossypol. The optical and chemical stability of the condensate of enantiomeric gossypols with the titled amine and the great difference in the Rf values on TLC and the solubilities in various solvents between the two diastereoisomeric condensates facilitate the separation.Therefore,the pure isomers can be easily obtained by means of chromatography or crystallization.
出处 《药学学报》 CAS CSCD 北大核心 1990年第6期430-434,共5页 Acta Pharmaceutica Sinica
关键词 棉酚 消旋反应 Gossypol (+)or (-)- Gossypol Threo (-)or (+)- 1- (p-nitrophenyl)-1, 3 - dihydroxy propylamine - 2
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参考文献4

  • 1司伊康,药学学报,1990年,25卷,423页
  • 2郑多楷,药学学报,1990年,25卷,417页
  • 3司伊康,中国科学.A,1986年,8期,850页
  • 4司伊康,科学通报,1983年,23卷,640页

同被引文献8

  • 1杨春梅,唐辉,顾承志,韩博,景文娟.光学活性棉酚衍生物的拆分及性质测定[J].山东医药,2006,46(35):1-2. 被引量:5
  • 2Ko C H,Shen S C,Yang L Y,et al. Gossyl:ol reduction of tumor growth through ROS-dependent mitochondria pathway in human coloreetal carcinorm cells[J]. Int J Cancer ,2007,121 (8) : 1670- 1679.
  • 3Catherine V P, Andrew D S, Marcus M R,et al. Oral gossypol in the treatment of patients with refractory metastatic breast cancer: A phase I/II clinical trial [ J ]. Breast Cancer Research and Treatment,2001,66(3) :239-248.
  • 4Baram N I,Ismailov A l,Ziyaev K L,et al. Biological activity of gossypol and its derivatives [ J]. Chem Nat Compd, 2004,40 ( 3 ) : 199-205.
  • 5Dao V T, Dowd M K, Martin M T, et al. Cytotoxicity of enantiomers of gossypol Schiff' s bases and optical stability of gossypolone [ J]. European Journal of Medicinal Chemistry, 2004,39: 619-624.
  • 6郑多楷,黄量,司伊康,等.制备光学活性棉酚的方法[P].CN:1033795,1987.
  • 7Fish R, Groundwater P, Morga J. The Photoepimerisation of Gossypol Schiff' s Bases [ J ]. Tetrahedron: Asymmetry, 1995,6: 873-876.
  • 8司伊康,郑多楷,黄量.消旋棉酚拆分的研究——Ⅲ.胺缩棉酚理化性质的研究[J].药学学报,1990,25(6):423-429. 被引量:5

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