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It is reported that replacing H atom of N -alkyl with D atom would improve drug pharmacokinetic properties. This paper further develops the diethylamine-d 10 synthetic process which uses ethanol-d 6 as the starting material, with an overall yield of more than 40% for the three reaction steps and the deuterium abundance of diethylamine-d 10 being more than 98%. These results are useful for development of novel deuterium drug candidates containing diethylamine-d 10 fragments., authors=LIU Zijie1 , YU Wenjun2 , XIE Xilei1 , LIU Gang1,2 , authorsList=LIU Zijie, YU Wenjun, XIE Xilei, LIU Gang, authorCompany=1. Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation; Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China;N -烷基的氢(H)原子替换为氘(D)原子, 可显著改善药物分子的药代动力学性质。本文发展了使用乙醇-d 6 为原料, 通过三步反应制得二乙胺-d 10 的合成方法, 总收率大于40%, 氘代丰率大于98%, 期望能够应用于新型氘代药物的研发过程中。, authors=刘子节1 , 于文俊2 , 解希雷1 , 刘刚1,2 , authorsList=刘子节, 于文俊, 解希雷, 刘刚, authorCompany=1. 中国医学科学院北京协和医学院药物研究所;活性物质发现与适药化研究北京市重点实验室, 北京100050;10 ), Keyword(id=1242133565652152457, tenantId=1146029695717560320, journalId=1146031591421210625, articleId=1242133562095378566, language=CN, orderNo=1, keyword=氘代), Keyword(id=1242133565761204364, tenantId=1146029695717560320, journalId=1146031591421210625, articleId=1242133562095378566, language=CN, orderNo=1, keyword=制备), Keyword(id=1242133566520369299, tenantId=1146029695717560320, journalId=1146031591421210625, articleId=1242133562095378566, language=EN, orderNo=1, keyword=diethylamine-d10 ), 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科技导报
| 研究论文 2015, 33(12): 15-18
氘代二乙胺的制备
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刘子节1 , 于文俊2 , 解希雷1 , 刘刚1,2
作者信息
1. 中国医学科学院北京协和医学院药物研究所;活性物质发现与适药化研究北京市重点实验室, 北京100050;
通讯作者:
刘刚, 教授, 研究方向为药物化学与化学生物学, 电子信箱:gangliu27@tsinghua.edu.cn
Preparation of diethylamine-d 10
Affiliations
出版时间: 2015-06-28
doi: 10.3981/j.issn.1000-7857.2015.12.001
文章导航
二乙胺是一种重要的有机化工原料, 常应用于医药中间体的合成;同时, 二乙胺基也常成为药物分子中重要的活性结构片段。将N -烷基的氢(H)原子替换为氘(D)原子, 可显著改善药物分子的药代动力学性质。本文发展了使用乙醇-d 6 为原料, 通过三步反应制得二乙胺-d 10 的合成方法, 总收率大于40%, 氘代丰率大于98%, 期望能够应用于新型氘代药物的研发过程中。
Diethylamine, one of the important organic chemicals, is widely used in preparation of pharmaceutical intermediates, and is often an important candidate of active fragments of drugs. It is reported that replacing H atom of N -alkyl with D atom would improve drug pharmacokinetic properties. This paper further develops the diethylamine-d 10 synthetic process which uses ethanol-d 6 as the starting material, with an overall yield of more than 40% for the three reaction steps and the deuterium abundance of diethylamine-d 10 being more than 98%. These results are useful for development of novel deuterium drug candidates containing diethylamine-d 10 fragments.
diethylamine-d10
/
deuterium
/
preparation
刘子节, 于文俊, 解希雷, 刘刚.
氘代二乙胺的制备.
科技导报,
2015
, 33
(12)
: 15
-18
.
DOI: 10.3981/j.issn.1000-7857.2015.12.001
LIU Zijie, YU Wenjun, XIE Xilei, LIU Gang.
Preparation of diethylamine-d 10 [J].
Science & Technology Review ,
2015
, 33
(12)
: 15
-18
.
DOI: 10.3981/j.issn.1000-7857.2015.12.001
2015年第33卷第12期
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文章信息
doi: 10.3981/j.issn.1000-7857.2015.12.001
接收时间：2015-04-23
首发时间：2015-07-15
出版时间：2015-06-28
收稿日期：2015-04-23
修回日期：2015-05-25
通讯作者:
刘刚, 教授, 研究方向为药物化学与化学生物学, 电子信箱:gangliu27@tsinghua.edu.cn
https://castjournals.cast.org.cn/joweb/kjdb/CN/10.3981/j.issn.1000-7857.2015.12.001
引用本文
BibTeX
2种不同金属材料的力学参数
科 属数 种数 占总种数比例 属 种数 占总种数比例 鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78 小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39 多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39 红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87 小菇属 Mycena 11 5.26 光柄菇属 Pluteus 5 2.39 红菇属 Russula 17 8.13 栓菌属 Trametes 5 2.39
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