Articles

Preparation of diethylamine-d10

  • LIU Zijie ,
  • YU Wenjun ,
  • XIE Xilei ,
  • LIU Gang
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  • 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;
    2. Tsinghua-Peking Center for Life Sciences; Department of Pharmacology and Pharmaceutical Sciences, School of Medicine, Tsinghua University, Beijing 100084, China

Received date: 2015-04-23

  Revised date: 2015-05-25

  Online published: 2015-07-15

Abstract

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.

Cite this article

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

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