Premium
Synthesis of 5‐hydroxy‐[6‐ 14 C]‐methyl‐2‐di‐n‐propylaminotetralin
Author(s) -
Koble Dale L.,
Fischer Lawrence J.
Publication year - 1984
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.2580210605
Subject(s) - chemistry , formylation , paraformaldehyde , yield (engineering) , chemical synthesis , agonist , radiosynthesis , stereochemistry , organic chemistry , catalysis , biochemistry , in vitro , in vivo , receptor , materials science , metallurgy , microbiology and biotechnology , biology
By an improved synthesis, 5‐hydroxy‐6‐methyl‐2‐di‐n‐propylaminotetralin (DK‐118), a dopamine agonist, has been obtained in only six steps and in greater than 10% overall yield. This new synthesis has been used for the preparation of 5‐hydroxy‐[6‐ 14 C]‐methyl‐2‐di‐n‐propylaminotetralin ( I ) to be used in metabolic studies. The 14 C‐radiolabel was introduced near the end of the synthesis by an ortho‐specific formylation procedure using 14 C‐paraformaldehyde.