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An efficient synthesis of deuterium‐labeled degarelix acetate, a third‐generation gonadotropin‐releasing hormone receptor antagonist
Author(s) -
Huang Yu,
Chen Jingshun,
Liu Baomin,
Wang Hua,
Zhang Lu,
Chen Zhengbang,
Zhang Yinsheng
Publication year - 2018
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3567
Subject(s) - chemistry , antagonist , deuterium , yield (engineering) , radiochemistry , receptor , biochemistry , physics , materials science , quantum mechanics , metallurgy
Degarelix acetate, a third‐generation gonadotropin‐releasing hormone receptor antagonist, shows great potential in the treatment of many androgen‐related diseases. To support clinical studies of degarelix acetate, deuterium‐labeled degarelix is highly desired for use as an internal standard. Using D 2 O/D 3 PO 4 as a deuterium source, 2‐amino‐3‐(naphthalen‐2‐yl)propanoic acid was converted to deuterated degarelix acetate in 13 steps and in 14% overall yield.