Iridium‐Catalysed C− H Borylation of Heteroarenes: Balancing Steric and Electronic Regiocontrol
The iridium‐catalysed borylation of aromatic C− H bonds has become the preferred method
for the synthesis of aromatic organoboron compounds. The reaction is highly efficient …
for the synthesis of aromatic organoboron compounds. The reaction is highly efficient …
Designing novel building blocks is an overlooked strategy to improve compound quality
Highlights•High quality building blocks can have a big impact on drug discovery.•
Commercial reagents do not satisfy our design criteria or provide sufficient SAR.•Design …
Commercial reagents do not satisfy our design criteria or provide sufficient SAR.•Design …
A close-up look at the chemical space of commercially available building blocks for medicinal chemistry
Y Zabolotna, DM Volochnyuk… - Journal of chemical …, 2021 - ACS Publications
The ability to efficiently synthesize desired compounds can be a limiting factor for chemical
space exploration in drug discovery. This ability is conditioned not only by the existence of …
space exploration in drug discovery. This ability is conditioned not only by the existence of …
Metal-Free Radical-Mediated C(sp3)–H Heteroarylation of Alkanes
X Shao, X Wu, S Wu, C Zhu - Organic Letters, 2020 - ACS Publications
Herein we disclose a metal-free, N/O-centered radical-promoted Minisci reaction, in which
the coupling of various heteroarenes with simple alkanes proceeds under mild conditions …
the coupling of various heteroarenes with simple alkanes proceeds under mild conditions …
Selective oxymetalation of terminal alkynes via 6-endo cyclization: mechanistic investigation and application to the efficient synthesis of 4-substituted isocoumarins
Y Kita, T Yata, Y Nishimoto, K Chiba, M Yasuda - Chemical Science, 2018 - pubs.rsc.org
The cyclization of heteroatom-containing alkynes with π acidic metal salts is an attractive
method to prepare heterocycles because the starting materials are readily available and the …
method to prepare heterocycles because the starting materials are readily available and the …
“Ring breaker”: neural network driven synthesis prediction of the ring system chemical space
A Thakkar, N Selmi, JL Reymond… - Journal of medicinal …, 2020 - ACS Publications
Ring systems in pharmaceuticals, agrochemicals, and dyes are ubiquitous chemical motifs.
While the synthesis of common ring systems is well described and novel ring systems can …
While the synthesis of common ring systems is well described and novel ring systems can …
Horner–Wadsworth–Emmons reaction as an excellent tool in the synthesis of fluoro-containing biologically important compounds
M Bilska-Markowska, M Kaźmierczak - Organic & Biomolecular …, 2023 - pubs.rsc.org
Selective introduction of a double bond motif into a multifunctional organic compound is
always a big challenge. The Horner–Wadsworth–Emmons reaction is one of the most …
always a big challenge. The Horner–Wadsworth–Emmons reaction is one of the most …
Iridium‐katalysierte C‐H‐Borylierung von Heteroarenen: Eine Balance zwischen sterischer and elektronischer Regiokontrolle
Abstract Die Ir‐katalysierte Borylierung aromatischer C‐H‐Bindungen ist heute die
bevorzugte Methode zur Synthese aromatischer Organoborverbindungen. Sie ist …
bevorzugte Methode zur Synthese aromatischer Organoborverbindungen. Sie ist …
Postmodification of the electronic properties by addition of π-stacking additives in N-heterocyclic carbene complexes with extended polyaromatic systems
A series of iridium complexes containing phenanthro [4, 5-abc] phenazino [11, 12-d]
imidazol-2-ylidene and acetonaphtho [1, 2-b] quinoxaline [11, 12-d] imidazol-2-ylidene …
imidazol-2-ylidene and acetonaphtho [1, 2-b] quinoxaline [11, 12-d] imidazol-2-ylidene …
Synthesis of 6‐Azaspiro [4.3] alkanes: Innovative Scaffolds for Drug Discovery
BA Chalyk, AA Isakov, MV Butko… - European Journal of …, 2017 - Wiley Online Library
New scaffolds for drug discovery, 6‐azaspiro [4.3] alkanes, have been synthesized in two
steps from four‐membered‐ring ketones: cyclobutanone, thienone, N‐Boc‐azetidinone …
steps from four‐membered‐ring ketones: cyclobutanone, thienone, N‐Boc‐azetidinone …