Conformational restriction: an effective tactic in'follow-on'-based drug discovery

Z Fang, Y Song, P Zhan, Q Zhang… - Future medicinal …, 2014 - Taylor & Francis
The conformational restriction (rigidification) of a flexible ligand has often been a commonly
used strategy in drug design, as it can minimize the entropic loss associated with the ligand …

Recent developments in the stereocontrolled synthesis of highly substituted cyclopentane core structures: from drug discovery research to natural product synthesis

B Heasley - Current Organic Chemistry, 2014 - ingentaconnect.com
The cyclopentane carbocyclic ring system, while ubiquitous in nature, is not usually
considered a privileged core structure for the development of a drug candidate due, in part …

Regioselective synthesis of polycyclic sulfones via radical-induced three-component bicyclization cascades

XY Qin, L He, J Li, WJ Hao, SJ Tu… - Chemical Communications, 2019 - pubs.rsc.org
New radical-triggered three-component bicyclization cascades of 2-alkynyl aryldiazonium
tetrafluoroborates with a sulfur dioxide surrogate DABCO·(SO2) 2 and internal alkynes such …

Photocatalytic three-component annulation enabling stereoselective generation of (Z)-thiochromene 1, 1-dioxides

KX Song, XY Qin, ZX Ma, FZ Geng, WJ Hao… - Organic Chemistry …, 2021 - pubs.rsc.org
A new photocatalytic three-component annulation of 2-alkynylaryldiazonium
tetrafluoroborates with γ-hydroxyl terminal alkynes and sodium metabisulfite is reported …

Advances in Synthesis of Enantioenriched Chiral Sulfones by Enantioselective Conjugate Addition Reactions

X Liang, Y Shen - Asian Journal of Organic Chemistry, 2022 - Wiley Online Library
Chiral sulfones, a class of organic compounds with broad application prospects in organic
synthesis and pharmaceutical chemistry, are an important part of building bioactive …

Inhibitors of the human neuraminidase enzymes

CW Cairo - MedChemComm, 2014 - pubs.rsc.org
The human neuraminidase enzymes (hNEU) are a family of four isoenzymes that hydrolyze
sialosides, including gangliosides and glycoproteins. These enzymes are proposed to play …

3-Sulfolenes and their derivatives: synthesis and applications

MG Brant, JE Wulff - Synthesis, 2016 - thieme-connect.com
The diverse substitution patterns available to 3-sulfolenes have long made them useful for
the preparation of multi-substituted 1, 3-diene equivalents. More recently, the 3-sulfolene …

Efficient synthesis of 3-sulfolenes from allylic alcohols and 1, 3-dienes enabled by sodium metabisulfite as a sulfur dioxide equivalent

HT Dang, VT Nguyen, VD Nguyen, HD Arman… - Organic & …, 2018 - pubs.rsc.org
We present herein an efficient and practical method for a gram scale synthesis of 3-
sulfolenes using sodium metabisulfite as a safe, inexpensive, and easy to handle sulfur …

An Asymmetric Allylic Alkylation–Smiles Rearrangement–Sulfinate Addition Sequence to Construct Chiral Cyclic Sulfones

QG Wang, QQ Zhou, JG Deng, YC Chen - Organic letters, 2013 - ACS Publications
An asymmetric allylic alkylation of Morita–Baylis–Hillman carbonates and β-keto sulfones
was investigated by the catalysis of modified cinchona alkaloids, whose products underwent …

[PDF][PDF] Synthesis of 3-aryl-6a-methyl-6-nitro-1-phenylhexahydrothieno [2, 3-d] pyrazole 4, 4-dioxides

VM Berestovitskaya, IE Efremova, LV Lapshina… - 2015 - dspace.spbu.ru
Synthesis of 3-aryl-6a-methyl-6-nitro-1-phenylhexahydrothieno[2,3-d]pyrazole 4,4-dioxides
Page 1 Mendeleev Commun., 2015, 25, 191–192 – 191 – Mendeleev Communications © 2015 …