The evolution of chemical high-throughput experimentation to address challenging problems in pharmaceutical synthesis

SW Krska, DA DiRocco, SD Dreher… - Accounts of chemical …, 2017 - ACS Publications
Conspectus The structural complexity of pharmaceuticals presents a significant challenge to
modern catalysis. Many published methods that work well on simple substrates often fail …

Chemistry informer libraries: conception, early experience, and role in the future of cheminformatics

SD Dreher, SW Krska - Accounts of Chemical Research, 2021 - ACS Publications
Conspectus The synthetic chemistry literature traditionally reports the scope of new methods
using simple, nonstandardized test molecules that have uncertain relevance in applied …

Anion-tuning of organozincs steering cobalt-catalyzed radical relay couplings

X Liu, H Chen, D Yang, B Hu, Y Hu, S Wang… - ACS …, 2023 - ACS Publications
A multicomponent sulfonylarylation reaction via cobalt-catalyzed alkene difunctionalizations
with sulfonyl chlorides and OPiv-supported organozinc reagents was reported. Herein …

Salt‐Stabilized Silylzinc Pivalates for Nickel‐Catalyzed Carbosilylation of Alkenes

J Wang, Z Duan, X Liu, S Dong, K Chen… - Angewandte …, 2022 - Wiley Online Library
We herein report the preparation of solid and salt‐stabilized silylzinc pivalates from the
corresponding silyllithium reagents via transmetalation with Zn (OPiv) 2. These resulting …

Cobalt-catalyzed electrophilic aminations with anthranils: an expedient route to condensed quinolines

J Li, E Tan, N Keller, YH Chen… - Journal of the …, 2018 - ACS Publications
The reaction of various organozinc pivalates with anthranils provides anilines derivatives,
which cyclize under acidic conditions providing condensed quinolines. Using alkenylzinc …

Decarboxylative Negishi coupling of redox‐active aliphatic esters by cobalt catalysis

XG Liu, CJ Zhou, E Lin, XL Han, SS Zhang… - Angewandte …, 2018 - Wiley Online Library
A cobalt‐catalyzed decarboxylative Negishi coupling reaction of redox‐active aliphatic
esters with organozinc reagents was developed. The method enabled efficient alkyl–aryl …

Recent progresses in the synthesis of functionalized isoxazoles

T Morita, S Yugandar, S Fuse, H Nakamura - Tetrahedron Letters, 2018 - Elsevier
Isoxazole is an important pharmacophore that is critical for biological activity. The isoxazole
ring ranks 33rd in frequency among the 351 ring systems found in marketed drugs, thus …

Salt-stabilized alkylzinc pivalates: versatile reagents for cobalt-catalyzed selective 1, 2-dialkylation

J Lin, K Chen, J Wang, J Guo, S Dai, Y Hu, J Li - Chemical Science, 2023 - pubs.rsc.org
The construction of Csp3–Csp3 bonds through Negishi-type reactions using alkylzinc
reagents as the pronucleophiles is of great importance for the synthesis of pharmaceuticals …

Organozinc pivalates for cobalt-catalyzed difluoroalkylarylation of alkenes

X Cheng, X Liu, S Wang, Y Hu, B Hu, A Lei… - Nature …, 2021 - nature.com
Installation of fluorine into pharmaceutically relevant molecules plays a vital role in their
properties of biology or medicinal chemistry. Direct difunctionalization of alkenes and 1, 3 …

Accessing three-dimensional molecular diversity through benzylic C–H cross-coupling

SJ Chen, CQ He, M Kong, J Wang, S Lin, SW Krska… - Nature …, 2023 - nature.com
Pharmaceutical discovery efforts rely on robust synthetic methods that rapidly access
diverse molecules. Cross-coupling reactions are the most widely used reactions, but these …