New synthetic routes to thyroid hormone analogs: d6-sobetirome, 3H-sobetirome, and the antagonist NH-3

AT Placzek, TS Scanlan - Tetrahedron, 2015 - Elsevier
New synthetic routes for the preparation of isotopically labeled versions of thyroid hormone
agonist sobetirome were developed using Knochel's iodine–magnesium exchange. A more
efficient synthesis of the thyroid hormone antagonist NH-3 was developed from a common
intermediate in the sobetirome route. Using the new synthetic routes, d 6-and 3 H-
sobetirome were prepared for their use in studying biodistribution and the cellular uptake of
sobetirome. The new route to NH-3 allows for a more rapid and efficient synthesis and …