Gram-Scale Laboratory Synthesis of TC AC 28, a High-Affinity BET Bromodomain Ligand

摘要

TC AC 28 , 6-(1H -Indol-4-yl)-8-methoxy-1-methyl-4H -[1,2,4]triazolo[4,3-a ][1,4]benzodiazepine-4-acetic acid methyl ester, has been synthesized on a near-gram scale in seven steps with notable improvements in the reported poor-yielding last two steps enabling this key chemical probe compound to be available for researchers.