Carbon‐14 Labeling Synthesis of RORγt Inhibitor JNJ‐61803534

• DOI: 10.1002/jlcr.4114
• Publication Date: 2024-05-28T04:23:25Z
• Authors: Fengbin Song; Rhys Salter; Lu Chen
• Keywords: Thiazole; Carbon fibers; Nitrile hydratase

ABSTRACT Carbon‐14 labeling synthesis of RORγt inhibitor JNJ‐61803534 ( 1 ) was accomplished in four steps with the C14 label located at thiazole‐2‐carboxamide carbon. The featured a highly efficient conversion nitrile [ 14 C]‐ 12 to ester 17 under mild conditions via an imidate intermediate, overcoming unsuccessful direct hydrolysis either acidic or basic conditions. Since carbon‐14 C]‐nitrile installation and subsequent C]‐carboxylic acid derivatives is common strategy, could be use for future syntheses.