Science & Technology Review
|
2015, 33(12): 15-18
• Articles •
Preparation of diethylamine-d10
Full
LIU Zijie, YU Wenjun, XIE Xilei, LIU Gang
Affiliations
Published: 2015-06-28
doi: 10.3981/j.issn.1000-7857.2015.12.001
Outline
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-d10 synthetic process which uses ethanol-d6 as the starting material, with an overall yield of more than 40% for the three reaction steps and the deuterium abundance of diethylamine-d10 being more than 98%. These results are useful for development of novel deuterium drug candidates containing diethylamine-d10 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-d10[J].
Science & Technology Review,
2015
, 33
(12)
: 15
-18
.
DOI: 10.3981/j.issn.1000-7857.2015.12.001
Year 2015 volume 33 Issue 12
PDF
656
200
Cite this Article
BibTeX
Article Info
doi: 10.3981/j.issn.1000-7857.2015.12.001
- Receive Date:2015-04-23
- Online Date:2015-07-15
- Published:2015-06-28