title: Solid-phase parallel synthesis of a tetrahydroindazolone library containing three unique core skeletons.
abstract: We have developed a practical strategy for the regioselective synthesis of a 1-(hetero)aryl-3-substituted tetrahydroindazolone library. The condensation of in situ generated arylhydrazine on solid supports with 2-acylcyclohexane-1,3-diones ensured the efficiency of solid-phase parallel synthesis. In addition, we introduced three unique core skeletons containing nitrophenyl, anilyl, and pyridyl groups to maximize the molecular diversity through a diverse display of polar surface area in 3D chemical space. A 162-membered drug-like tetrahydroindazolone library was constructed in an average purity of 92% without further purification.
authors: Department of Chemistry, Seoul National University, 151-747 Seoul, South Korea.
authors: Jonghoon
authors: J
authors: Kim
authors: Heebum
authors: H
authors: Song
authors: Seung Bum
authors: SB
authors: Park