Palladium-catalyzed enol/enolate directed oxidative annulation: functionalized naphthofuroquinone synthesis and bioactivity evaluation

2019 ◽  
Vol 55 (98) ◽  
pp. 14729-14732 ◽  
Author(s):  
Shuaipeng Lv ◽  
Haitao Liu ◽  
Jie Kang ◽  
Yun Luo ◽  
Ting Gong ◽  
...  
Keyword(s):  
Late Stage ◽  
Lead Compound ◽  
Heterocycle Synthesis ◽  
Palladium Catalyzed ◽  
Catalytic Processes

Diverse naphthoquinone-containing heterocycle synthesis has been developed via enol/enolate-directed palladium catalytic processes together with late-stage functionalization and lead compound development.

Sequential C-Selective Difluoromethylation/Pd-Catalyzed Decarboxylative Protonation: An Efficient Access to Tertiary Difluoromethylated Scaffolds

2019 ◽  
Author(s):  
Nicolas Duchemin ◽  
Roberto Buccafusca ◽  
Marc Daumas ◽  
Vincent Ferey ◽  
Stellios Arseniyadis
Keyword(s):  
Drug Development ◽  
Late Stage ◽  
Efficient Access ◽  
Palladium Catalyzed ◽  
General Method

We report here a general method that allows a highly straightforward access to tertiary difluoromethylated compounds. The strategy relies on a two-step sequence featuring a C-selective electrophilic difluoromethylation and an unprecedented palladium-catalyzed decarboxylative protonation. Considering the generality of the method and the attractive properties offered by the difluoromethyl group, this approach provides a valuable tool for late-stage functionalization and drug development.<br>

scholarly journals Palladium-Catalyzed Late-Stage Direct Arene Cyanation

Chem ◽  
2019 ◽  
Vol 5 (1) ◽  
pp. 97-107 ◽  
Author(s):  
Da Zhao ◽  
Peng Xu ◽  
Tobias Ritter
Keyword(s):  
Late Stage ◽  
Palladium Catalyzed

R75761, a lead compound for the development of antiviral drugs in late stage poliomyelitis eradication strategies and beyond

2008 ◽  
Vol 78 (3) ◽  
pp. 278-281 ◽  
Author(s):  
Bert Thys ◽  
Armando M. De Palma ◽  
Johan Neyts ◽  
Koen Andries ◽  
Raf Vrijsen ◽  
...  
Keyword(s):  
Late Stage ◽  
Antiviral Drugs ◽  
Lead Compound

scholarly journals Fully Substituted Pyrazoles Assisted Palladium-Catalyzed Late-Stage Arylation of C(sp2)—H Bond

2020 ◽  
Vol 40 (12) ◽  
pp. 4305
Author(s):  
Xiaopan Fu ◽  
Yangyang Wang ◽  
Jinyue Yang ◽  
Gaorong Wu ◽  
Chengcai Xia ◽  
...  
Keyword(s):  
Late Stage ◽  
Palladium Catalyzed ◽  
Substituted Pyrazoles

scholarly journals Synthesis and Anti-Tuberculosis Activity of Olivacine and Oxygenated Derivatives

2018 ◽  
Author(s):  
Ulrike Schmidt ◽  
Gabriele Theumer ◽  
Anne Jäger ◽  
Olga Kataeva ◽  
Baojie Wan ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Late Stage ◽  
Pyrrole Ring ◽  
Palladium Catalyzed ◽  
Tuberculosis Activity

The tetracyclic pyrido[4,3-b]carbazole olivacine and four of its oxygenated derivatives have been synthesized by a late-stage palladium-catalyzed Heck-type cyclization of the pyrrole ring as key step. In a test for inhibition of the growth of Mycobacterium tuberculosis 9-methoxyolivacine showed the most significant anti-TB activity with an MIC90 value of 1.5 &mu;M.

Ligand-Free Palladium-Catalyzed Carbonylative Suzuki Couplings of Vinyl Iodides with Arylboronic Acids under Substoichiometric Base Conditions

Synlett ◽  
2021 ◽  
Author(s):  
Zhiyuan Yang ◽  
Pei-Xue Gong ◽  
Junjie Chen ◽  
Jie Zhang ◽  
Xu Gong ◽  
...  
Keyword(s):  
Late Stage ◽  
Ambient Pressure ◽  
Complex Molecule ◽  
Arylboronic Acids ◽  
Simple Protocol ◽  
Ligand Free ◽  
Reaction Proceeds ◽  
Palladium Catalyzed ◽  
Vinyl Iodides

A ligand-free palladium-catalyzed carbonylation of vinyl iodides with arylboronic acids allowing for the synthesis of chalcones and α-branched enones has been established. This reaction proceeds smoothly under ambient pressure and temperature and even use of substoichiometric base renders the transformation to work well. Importantly, this mild, efficient, operationally simple protocol is suitable for the late-stage functionalization of an epiandrosterone-derived complex molecule.

Late‐Stage Peptide Macrocyclization by Palladium‐Catalyzed Site‐Selective C−H Olefination of Tryptophan

2020 ◽  
Vol 132 (34) ◽  
pp. 14794-14800
Author(s):  
Zengbing Bai ◽  
Chuangxu Cai ◽  
Wangjian Sheng ◽  
Yuxiang Ren ◽  
Huan Wang
Keyword(s):  
Late Stage ◽  
Palladium Catalyzed ◽  
Site Selective
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