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Synthesis of 2‐methyl‐2‐[[(7‐methyl‐7 H ‐benzo[ c ]carbazol‐10‐yl)[ 14 C]methyl[amino]‐1,3‐propanediol mesylate — a potential antitumor agent
Author(s) -
Hill John A.,
Eaddy John F.
Publication year - 1994
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.2580340803
Subject(s) - chemistry , mesylate , formylation , carbazole , reductive amination , amination , propanediol , stereochemistry , indole test , chemical synthesis , organic chemistry , in vitro , biochemistry , catalysis
2‐Methyl‐2‐[[(7‐methyl‐ 7H ‐benzo[c]carbazol‐10‐yl)methyl]amino]‐1,3‐propanediol ( 1 , 7U85) was synthesized as the mesylate salt in the [ 14 C]‐labelled form with specific activity 48.4 mCi/mmol suitable for metabolism and tissue distribution studies in animals The synthetic sequence involved the regiospecific synthesis of a bromobenzo[c]carbazole by a modified Fischer indole synthesis, formylation by a Bouveault reaction, and reductive amination. The radiochemical purity was > 97.3%.