| 以鸟苷为原料合成巴豆苷 |
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| 引用本文： | 孙莉萍,焦黎明,杨政楠,潘心,夏然,陈磊山.以鸟苷为原料合成巴豆苷[J].精细石油化工,2021,38(2):63-67. |
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| 作者姓名： | 孙莉萍 焦黎明 杨政楠 潘心 夏然 陈磊山 |
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| 作者单位： | 新乡学院生命科学与基础医学学院,河南新乡453003;新乡学院药学院,河南新乡453003 |
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| 基金项目： | 河南省高等学校青年骨干教师培养计划;大学生创新创业训练国家级项目;国家自然科学基金 |
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| 摘 要： | 为了解决巴豆苷合成时原料价格高的问题,以廉价易得的鸟苷为原料,用乙酰基保护糖环上的羟基,再和POCl 3反应,将6位羰基转化为氯原子,继而在亚硝酸异戊酯作用下发生重氮化反应,将2位氨基转化为羟基,最后在饱和的NH3/CH3OH溶液中将6位氯原子氨解转化为氨基,同时脱除乙酰基,以4步和62%的总收率得到巴豆苷。该方法高效、简便,反应规模可以扩大到200 g,具有一定的应用前景。
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| 关 键 词： | 鸟苷 巴豆苷 重氮化反应 合成方法 |
THE SYNTHESIS OF CROTONOSIDE FROM GUANOSINE |
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| Sun Liping,Jiao Liming,Yang Zhengnan,Pan Xin,Xia Ran,Chen Leishan.THE SYNTHESIS OF CROTONOSIDE FROM GUANOSINE[J].Speciality Petrochemicals,2021,38(2):63-67. |
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| Authors: | Sun Liping Jiao Liming Yang Zhengnan Pan Xin Xia Ran Chen Leishan |
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| Affiliation: | (School of Iife Sciences&Basic Medicine,Xinxiang 453003,He’nan,China;School of pharmacy,Xinxiang University,Xinxiang 453003,He’nan,China) |
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| Abstract: | In order to avoid high price of raw materials in the traditional synthesis of Crotonoside,This paper reported the synthesis of Crotonoside from guanosine with 4 steps and 62%total yield.Firstly,the hydroxyl groups of guanosine were protected by acetyl groups and then 6-carbonyl group was converted into chloride by POCl 3.Secondly,2-NH 2 was converted into—OH via diazotization with isoamyl nitrite.Finally,6-Cl was ammonolysized to—NH 2 in saturated NH3/CH3OH solution,and acetyl groups were removed at the same time.This method was efficient,simple and.The reaction scale could be expanded to 200 g,which made this route more attractive for industrial application. |
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| Keywords: | guanosine Crotonoside diazotization synthetic methods |
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