A convergent synthesis of (S)-β-methyl-2-aryltryptamine based gonadotropin releasing hormone antagonists

Abstract A practical synthesis of ( S )-β-methyl-2-aryltryptamine based gonadotropin releasing hormone antagonists which features a palladium-catalyzed Larock indole synthesis and a palladium-catalyzed Suzuki–Miyaura sequence to install the 2-position aryl substituent is reported.