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Solid‐Phase Parallel Synthesis of a Tetrahydroindazolone Library Containing Three Unique Core Skeletons
Author(s) -
Kim Jonghoon,
Song Heebum,
Park Seung Bum
Publication year - 2011
Publication title -
chemistry – an asian journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.18
H-Index - 106
eISSN - 1861-471X
pISSN - 1861-4728
DOI - 10.1002/asia.201100145
Subject(s) - core (optical fiber) , computer science , phase (matter) , chemistry , telecommunications , organic chemistry
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.