Carbon-14 Labeling Synthesis of RORγt Inhibitor JNJ-61803534.
J Labelled Comp Radiopharm
; 67(8): 288-294, 2024 Jun 30.
Article
in En
| MEDLINE
| ID: mdl-38803015
ABSTRACT
Carbon-14 labeling synthesis of RORγt inhibitor JNJ-61803534 (1) was accomplished in four steps with the C14 label located at the thiazole-2-carboxamide carbon. The synthesis featured a highly efficient conversion of nitrile [14C]-12 to ester [14C]-17 under mild conditions via an imidate intermediate, overcoming the unsuccessful direct hydrolysis of nitrile 12 under either acidic or basic conditions. Since carbon-14 labeling via [14C]-nitrile installation and subsequent conversion to [14C]-carboxylic acid derivatives is a common labeling strategy, an efficient conversion of a nitrile to an ester under mild conditions could be of use for the future C14 labeling syntheses.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Carbon Radioisotopes
/
Nuclear Receptor Subfamily 1, Group F, Member 3
Language:
En
Journal:
J Labelled Comp Radiopharm
Year:
2024
Document type:
Article