[1]方波,陶凌晖,周向东,等.树化胺基甾醇类似物6β-丁胺基胆甾-3β, 5α-二醇的合成[J].陆军军医大学学报(原第三军医大学学报),2010,32(10):1051-1054.
 Fang Bo,Tao Linghui,Zhou Xiangdong,et al.Synthesis of 6β-butylaminocholestan-3β, 5α-diol, an analogue of anti-tumoral dendrogenin[J].J Amry Med Univ (J Third Mil Med Univ),2010,32(10):1051-1054.
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陆军军医大学学报(原第三军医大学学报)[ISSN:1000-5404/CN:51-1095/R]

卷:
32卷
期数:
2010年第10期
页码:
1051-1054
栏目:
论著
出版日期:
2010-05-30

文章信息/Info

Title:
Synthesis of 6β-butylaminocholestan-3β, 5α-diol, an analogue of anti-tumoral dendrogenin
作者:
方波陶凌晖周向东周成合
西南大学化学化工学院生物有机药物化学实验室;第三军医大学药学院药物化学教研室
Author(s):
Fang Bo Tao Linghui Zhou Xiangdong Zhou Chenghe
Laboratory of Bioorganic & Medicinal Chemistry, School of Chemistry and Chemical Engineering, Southwest University, Chongqing, 400715; Department of Medicinal Chemistry, College of Pharmacy, Third Military Medical University, Chongqing, 400038, China
关键词:
胆固醇树化胺基甾醇亚胺化-还原两步一锅法抗肿瘤
Keywords:
cholesterol dendrogenins imidation-reduction of one-pot two steps antitumor
分类号:
R914.5;O629.21;R979.1
文献标志码:
A
摘要:
目的   新法合成新型抗肿瘤树化胺基甾醇类似物6β-丁胺基胆甾-3β,5α-二醇。   方法   以胆固醇为原料,3β,5α-二羟基胆甾-6-酮为关键中间体,亚胺化-还原为关键步骤,经5步反应合成6β-丁胺基胆甾-3β,5α-二醇。   结果   以62%的总收率合成了目标化合物,其结构与实测MS(476)、HRMS(476.446 5)、[α]25D(-57.0°)、IR(3 387)、1HNMR[2.67~2.61(1H, m, 6α-H)]、13CNMR和元素分析一致。   结论   以本法合成6β-丁胺基胆甾-3β,5α-二醇,原料廉价易得、总收率高、易于工业化。
Abstract:
Objective   To synthesize 6β-butylaminocholestan-3β,5α-diol, a new analogue of anti-tumoral dendrogenin with a new method.    Methods   6β-butylaminocholestan-3β,5α-diol was synthesized in 5 steps using cholesterol as the starting material, 3β,5α-dihydroxyl-cholestan-6-one as the key intermediate and imidation-reduction of one-pot 2 steps as the key steps.    Results   The target compound was synthesized in a total yield of 62% and its structure were consistent with MS (476), HRMS (476.446 5), [α]25D(-57.0°), IR (3387), 1HNMR [2.67~2.61 (1H, m, 6α-H)], 13CNMR spectrum and elemental analyses.    Conclusion   Our synthetic route to 6β-butylaminocholestan-3β, 5α-diol is characterized by easily available and cheap starting material, high total yield and easy industrialization.

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更新日期/Last Update: 2010-05-20