An efficient synthesis of deuterium‐labeled degarelix acetate, a third‐generation gonadotropin‐releasing hormone receptor antagonist

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.