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- Title
Synthesis of Complex Druglike Molecules by the Use of Highly Functionalized Bench-Stable Organozinc Reagents.
- Authors
Greshock, Thomas J.; Moore, Keith P.; McClain, Ray T.; Bellomo, Ana; Chung, Cheol K.; Dreher, Spencer D.; Kutchukian, Peter S.; Peng, Zhengwei; Davies, Ian W.; Vachal, Petr; Ellwart, Mario; Manolikakes, Sophia M.; Knochel, Paul; Nantermet, Philippe G.
- Abstract
The reactivity of a representative set of 17 organozinc pivalates with 18 polyfunctional druglike electrophiles (informers) in Negishi cross-coupling reactions was evaluated by high-throughput experimentation protocols. The high-fidelity scaleup of successful reactions in parallel enabled the isolation of sufficient material for biological testing, thus demonstrating the high value of these new solid zinc reagents in a drug-discovery setting and potentially for many other applications in chemistry. Principal component analysis (PCA) clearly defined the independent roles of the zincates and the informers toward druggable-space coverage.
- Subjects
ORGANOZINC compounds; BENZYLIC group; HETEROCHAIN polymers; ELECTROPHILES; COUPLING reactions (Chemistry)
- Publication
Angewandte Chemie, 2016, Vol 128, Issue 44, p13918
- ISSN
0044-8249
- Publication type
Article
- DOI
10.1002/ange.201604652