Three-dimensional saturated C(sp3)-rich bioisosteres for benzene

J Tsien, C Hu, RR Merchant, T Qin - Nature Reviews Chemistry, 2024 - nature.com
Benzenes, the most ubiquitous structural moiety in marketed small-molecule drugs, are
frequently associated with poor 'drug-like'properties, including metabolic instability, and poor …

General Synthesis of 3‐Azabicyclo [3.1. 1] heptanes and Evaluation of Their Properties as Saturated Isosteres

D Dibchak, M Snisarenko, A Mishuk… - Angewandte …, 2023 - Wiley Online Library
A general approach to 3‐azabicyclo [3.1. 1] heptanes by reduction of spirocyclic oxetanyl
nitriles was developed. The mechanism, scope, and scalability of this transformation were …

Fluoroalkyl‐Containing 1, 2‐Disubstituted Cyclobutanes: Advanced Building Blocks for Medicinal Chemistry

OP Demchuk, OV Hryshchuk… - European Journal of …, 2021 - Wiley Online Library
Abstract Synthesis of previously unavailable 1, 2‐disubstituted cyclobutane building blocks
bearing mono‐, di‐and trifluoromethyl groups are disclosed. The key steps included …

Novel approach to saturated amino acid derivatives with isolated (hetero)cyclic rings via the hydrogenation of dienes

EV Verner, BV Vashchenko, B Sosunovych… - Chemistry of …, 2023 - Springer
Synthesis of amino acids with isolated saturated (hetero) carbocyclic scaffold was disclosed.
The method relied on Suzuki cross-coupling reaction of heteroacycloalkene triflates and N …

Multigram Synthesis of 3‐Azabicyclo [3.1. 1] heptane Derivatives Including Bicyclic Thalidomide Analogs

V Lysenko, A Portiankin, O Shyshlyk… - European Journal of …, 2024 - Wiley Online Library
An efficient approach to the multigram synthesis of 3‐azabicyclo [3.1. 1] heptanes is
described. The method relied on the intramolecular imide formation in the properly 1, 3 …

4‐(Di‐/Trifluoromethyl)‐2‐heterabicyclo [2.1. 1] hexanes: Advanced Fluorinated Phenyl Isosteres and Proline analogues

AA Homon, OV Hryshchuk… - European Journal of …, 2021 - Wiley Online Library
A gram‐scale synthesis, physico‐chemical characterization, and lead‐likeness assessment
of 4‐di/trifluoromethyl‐2‐heterabicyclo [2.1. 1] hexanes as fluorinated bicyclic proline …

Unexpected Discovery of Saturated Pyridine Mimetics

D Dibchak, M Snisarenko, A Mishuk, O Shablykin… - 2023 - chemrxiv.org
A general approach to 3-azabicyclo [3.1. 1] heptanes was unexpectedly discovered. The
mechanism, scope, and scalability of this method were studied. The core was incorporated …

Monoprotected Diamines Derived from 1, 5‐Disubstituted (Aza) spiro [2.3] hexane Scaffolds

A Malashchuk, AV Chernykh… - European Journal of …, 2021 - Wiley Online Library
Synthesis of monoprotected diamines derived from 1, 5‐disubstituted spiro [2.3] hexane and
5‐azaspiro [2.3] hexane scaffolds is described. In both cases, the method relied on the …

[PDF][PDF] ФЕДЕРАЛЬНОЕ ГОСУДАРСТВЕННОЕ БЮДЖЕТНОЕ УЧРЕЖДЕНИЕ НАУКИ НОВОСИБИРСКИЙ ИНСТИТУТ ОРГАНИЧЕСКОЙ ХИМИИ ИМ. НН …

ЮВ Хорошунова - web3.nioch.nsc.ru
Актуальность темы исследования. Одним из современных подходов к исследованию
пространственной структуры биомакромолекул (белков, нуклеиновых кислот, их …

Synthesis of novel α-trifluoromethyl cyclobutane-containing building blocks

AA Homon, L Shynder, OV Hryshchuk… - Ukrainica …, 2022 - bioorganica.com.ua
Four new cyclobutane-containing building blocks were synthesized on a multigram scale
starting from 3-methylene-1-(trifluoromethyl) cyclobutane-1-carbonitrile and 3-methylene-1 …