期刊
ACS COMBINATORIAL SCIENCE
卷 14, 期 11, 页码 621-630出版社
AMER CHEMICAL SOC
DOI: 10.1021/co300098v
关键词
Povarov reaction; chiral urea; tetrahydroquinoline; asymmetric; solid-phase
资金
- NIGMS [P50 GM069721]
- NIH [RL1CA133834, RL1HG004671, RL1GM084437, UL1DE019585]
A 2328-membered library of 2,3,4-trisubstituted tetrahydroquinolines was produced using a combination of solution- and solid-phase synthesis techniques. A tetrahydroquinoline (THQ) scaffold was prepared via an asymmetric Povarov reaction using cooperative catalysis to generate three contiguous stereogenic centers. A matrix of 4 stereoisomers of the THQ scaffold was prepared to enable the development of stereo/structure-activity relationships (SSAR) upon biological testing. A sparse matrix design strategy was employed to select library members to be synthesized with the goal of generating a diverse collection of tetrahydroquinolines with physicochemical properties suitable for downstream discovery.
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