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Title:
PREPARATION METHOD FOR DEUTERATED COMPOUND
Document Type and Number:
WIPO Patent Application WO/2017/045648
Kind Code:
A1
Abstract:
The present invention relates to the field of chemical synthesis, and specifically to a preparation method for a deuterated compound. The preparation method comprises: converting a non-deuterated compound at least containing one structural element having a C-N-X formula into a corresponding deuterated compound in the presence of a deuterium source, wherein X indicates nitroso, nitro, hydroxy, cyan or alogen, the used deuterium source is selected from heavy water or deuterated alcohol, and the deuterium source is easy to obtain; the cost is low, the operation is simple and convenient, the preparation is easy, the deuteration time is short, the deuteration rate is high, the primary deuteration rate can be up to above 90 percent, a deuteration process has no use of high-toxicity reagent, and the preparation method is green and environment-friendly, and is particularly suitable for being applied to develop deuterated medicine.

Inventors:
ZHANG YINSHENG (CN)
GAO YONG (CN)
LIU YINGSHUAI (CN)
LIN ZHIQIANG (CN)
Application Number:
PCT/CN2016/099239
Publication Date:
March 23, 2017
Filing Date:
September 18, 2016
Export Citation:
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Assignee:
CHIA TAI TIANQING PHARMACEUTICAL GROUP CO LTD (CN)
International Classes:
C07C243/04; C07C211/48; C07D205/04; C07D213/74; C07D215/58; C07D217/02; C07D241/54; C07D295/30; C07D401/04; C07D471/04
Domestic Patent References:
WO2014081816A12014-05-30
Foreign References:
CN102190587A2011-09-21
Other References:
D. ROGIC ET AL.: "SYNTHESES DE PYRROLIDINES DEUTERIEES", JOURNAL OF LABELLED COMPOUNDS, vol. 10, no. 4, 31 December 1974 (1974-12-31), pages 655 - 661
H. CERECETTO ET AL.: "Mass Spectrometry of 1, 2, 5-oxadiazole N-Oxide Derivatives. Use of Deuterated Analogues in Fragmentation Pattern Studies", JOURNAL OF THE BRAZILIAN CHEMICAL SOCIETY, vol. 15, no. 2, 31 December 2004 (2004-12-31), pages 232 - 240, XP055371810
DATABASE REGISTRY STRUCTURE RESEAR 18 September 2011 (2011-09-18), "2, 2, 6, 6-Tetradeuterio-1-nitrosopiperidine-3-carboxylic acid", retrieved from STN Database accession no. 1329834-25-4
Attorney, Agent or Firm:
LINDA LIU & PARTNERS (CN)
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