Emerging building blocks for medicinal chemistry: recent synthetic advances

OO Grygorenko, DM Volochnyuk… - European Journal of …, 2021 - Wiley Online Library
Current medicinal chemistry relies heavily on the quality of building blocks, ie reagents used
to introduce chemical diversity into the target molecules. The last decade witnessed an …

Saturated boronic acids, boronates, and trifluoroborates: an update on their synthetic and medicinal chemistry

DM Volochnyuk, AO Gorlova… - Chemistry–A European …, 2021 - Wiley Online Library
This review discusses recent advances in the chemistry of saturated boronic acids,
boronates, and trifluoroborates. Applications of the title compounds in the design of boron …

A comprehensive discovery platform for organophosphorus ligands for catalysis

T Gensch, G dos Passos Gomes… - Journal of the …, 2022 - ACS Publications
The design of molecular catalysts typically involves reconciling multiple conflicting property
requirements, largely relying on human intuition and local structural searches. However, the …

Automated iterative Csp3–C bond formation

DJ Blair, S Chitti, M Trobe, DM Kostyra, HMS Haley… - Nature, 2022 - nature.com
Fully automated synthetic chemistry would substantially change the field by providing broad
on-demand access to small molecules. However, the reactions that can be run …

Desymmetrization of Vicinal Bis (boronic) Esters by Enantioselective Suzuki–Miyaura Cross-Coupling Reaction

M Zhang, PS Lee, C Allais, RA Singer… - Journal of the …, 2023 - ACS Publications
The development of an enantioselective catalytic Suzuki–Miyaura reaction that applies to
meso 1, 2-diborylcycloalkanes is described. This reaction provides a modular route to …

Copper-catalyzed stereospecific transformations of alkylboronic esters

N Xu, H Liang, JP Morken - Journal of the American Chemical …, 2022 - ACS Publications
Copper-catalyzed stereospecific cross-couplings of boronic esters are reported. Boron “ate”
complexes derived from pinacol boronic esters and tert-butyl lithium undergo stereospecific …

Stereoselective Diboration of Spirocyclobutenes: A Platform for the Synthesis of Spirocycles with Orthogonal Exit Vectors

L Nóvoa, L Trulli, A Parra, M Tortosa - Angewandte Chemie, 2021 - Wiley Online Library
The diastereo‐and enantioselective diboration of spirocyclobutenes provides a platform for
the rapid preparation of a wide variety of chiral spirocyclic building blocks. The …

Stereoselectivity in Pd-catalysed cross-coupling reactions of enantioenriched nucleophiles

X Ma, B Murray, MR Biscoe - Nature Reviews Chemistry, 2020 - nature.com
Advances in Pd-catalysed cross-coupling reactions have facilitated the development of
stereospecific variants enabling the use of configurationally stable, enantioenriched, main …

Stereospecific acylative Suzuki–Miyaura cross-coupling: general access to optically active α-aryl carbonyl compounds

B Roh, AO Farah, B Kim, T Feoktistova… - Journal of the …, 2023 - ACS Publications
A novel strategy for the stereospecific Pd-catalyzed acylative cross-coupling of
enantiomerically enriched alkylboron compounds has been developed. The protocol …

Isolation and characterization of heteroleptic mononuclear palladium (I) complexes

GN Tran, BS Bouley, LM Mirica - Journal of the American …, 2022 - ACS Publications
Catalytic transformations involving Pd (0)/Pd (II) catalytic cycles are very well known, and
processes involving high-valent Pd (III) and Pd (IV) and low-valent Pd (I) intermediates have …