Three-dimensional saturated C(sp3)-rich bioisosteres for benzene
Benzenes, the most ubiquitous structural moiety in marketed small-molecule drugs, are
frequently associated with poor 'drug-like'properties, including metabolic instability, and poor …
frequently associated with poor 'drug-like'properties, including metabolic instability, and poor …
Photochemistry in medicinal chemistry and chemical biology
Photochemistry has emerged as a transformative force in organic chemistry, significantly
expanding the chemical space accessible for medicinal chemistry. Light-induced reactions …
expanding the chemical space accessible for medicinal chemistry. Light-induced reactions …
Catalytic formal [2π+ 2σ] cycloaddition of aldehydes with bicyclobutanes: expedient access to polysubstituted 2‐oxabicyclo [2.1. 1] hexanes
Y Liang, F Paulus, CG Daniliuc… - Angewandte Chemie …, 2023 - Wiley Online Library
Synthesis of bicyclic scaffolds has attracted tremendous attention because they are playing
an important role as saturated bioisosteres of benzenoids in modern drug discovery. Here …
an important role as saturated bioisosteres of benzenoids in modern drug discovery. Here …
Silver‐catalyzed dearomative [2π+ 2σ] cycloadditions of indoles with bicyclobutanes: access to indoline fused bicyclo [2.1. 1] hexanes
L Tang, Y **ao, F Wu, JL Zhou, TT Xu… - Angewandte Chemie …, 2023 - Wiley Online Library
Abstract Bicyclo [2.1. 1] hexanes (BCHs) are becoming ever more important in drug design
and development as bridged scaffolds that provide underexplored chemical space, but are …
and development as bridged scaffolds that provide underexplored chemical space, but are …
Synthesis of 1-(halo) alkyl-3-heteroaryl bicyclo [1.1. 1] pentanes enabled by a photocatalytic minisci-type multicomponent reaction
J Zhu, Y Hong, Y Wang, Y Guo, Y Zhang, Z Ni… - ACS …, 2024 - ACS Publications
Aryl-substituted bicyclo [1.1. 1] pentane (BCP-aryl) derivatives represent the most important
bioisosteres of biaryl scaffolds and widely exist in numerous complex pharmaceutical …
bioisosteres of biaryl scaffolds and widely exist in numerous complex pharmaceutical …
Eu(OTf)3‐Catalyzed Formal Dipolar [4π+2σ] Cycloaddition of Bicyclo‐[1.1.0]butanes with Nitrones: Access to Polysubstituted 2‐Oxa‐3‐azabicyclo[3.1.1]heptanes
J Zhang, JY Su, H Zheng, H Li… - Angewandte Chemie, 2024 - Wiley Online Library
Herein, we have synthesized multifunctionalized 2‐oxa‐3‐azabicyclo [3.1. 1] heptanes,
which are considered potential bioisosteres for meta‐substituted arenes, through Eu (OTf) 3 …
which are considered potential bioisosteres for meta‐substituted arenes, through Eu (OTf) 3 …
Silver‐Enabled Cycloaddition of Bicyclobutanes with Isocyanides for the Synthesis of Polysubstituted 3‐Azabicyclo [3.1. 1] heptanes
Y Liang, R Nematswerani, CG Daniliuc… - Angewandte …, 2024 - Wiley Online Library
Synthesis of bicyclic scaffolds has emerged as an important research topic in modern drug
development because they can serve as saturated bioisosters to enhance the …
development because they can serve as saturated bioisosters to enhance the …
Skeletal editing approach to bridge-functionalized bicyclo [1.1. 1] pentanes from azabicyclo [2.1. 1] hexanes
BA Wright, A Matviitsuk, MJ Black… - Journal of the …, 2023 - ACS Publications
Azabicyclo [2.1. 1] hexanes (aza-BCHs) and bicyclo [1.1. 1] pentanes (BCPs) have emerged
as attractive classes of sp 3-rich cores for replacing flat, aromatic groups with metabolically …
as attractive classes of sp 3-rich cores for replacing flat, aromatic groups with metabolically …
General and modular route to (halo) alkyl BCP-heteroaryls enabled by α-aminoalkyl radical-mediated halogen-atom transfer
Y Guo, J Zhu, Y Wang, Y Li, H Hu, P Zhang, J Xu… - ACS …, 2023 - ACS Publications
Synthesis of bicyclo [1.1. 1] pentane (BCP) heteroaryls continues to be a part of the most
important tasks in organic synthesis because they are a significant class of bioisosteres with …
important tasks in organic synthesis because they are a significant class of bioisosteres with …
Double strain-release [2π+ 2σ]-photocycloaddition
In pursuit of potent pharmaceutical candidates and to further improve their chemical traits,
small ring systems can serve as a potential starting point. Small ring units have the …
small ring systems can serve as a potential starting point. Small ring units have the …