Electrocatalytic three-component annulation-halosulfonylation of 1,6-enynes toward 1-indanones using sodium halides as both halogen sources and electrolytes

2020 ◽  
Vol 22 (13) ◽  
pp. 4259-4269 ◽  
Author(s):  
Tian-Shu Zhang ◽  
Wen-Juan Hao ◽  
Rong Wang ◽  
Shi-Chao Wang ◽  
Shu-Jiang Tu ◽  
...  
Keyword(s):  
Stereoselective Synthesis ◽  
Environmentally Benign ◽  
Sodium Halides

A new electrochemically induced three-component annulation-halosulfonylation of 1,6-enynes has been developed for stereoselective synthesis of 33 examples of 1-indanones with generally good yields under environmentally benign conditions.

scholarly journals Synthesis and Evaluation of 3-Halobenzo[b]thiophenes as Potential Antibacterial and Antifungal Agents

2021 ◽  
Vol 15 (1) ◽  
pp. 39
Author(s):  
Prerna J. Masih ◽  
Tanay Kesharwani ◽  
Elivet Rodriguez ◽  
Mia A. Vertudez ◽  
Mina L. Motakhaveri ◽  
...  
Keyword(s):  
Antimicrobial Activities ◽  
Environmentally Benign ◽  
Health Concern ◽  
Gram Positive Bacteria ◽  
Sodium Halides ◽  
Thiophene Derivatives ◽  
Kill Curve ◽  
High Yields ◽  
Antibacterial And Antifungal ◽  
Time Kill

The global health concern of antimicrobial resistance has harnessed research interest to find new classes of antibiotics to combat disease-causing pathogens. In our studies, 3-halobenzo[b]thiophene derivatives were synthesized and tested for their antimicrobial activities using the broth microdilution susceptibility method. The 3-halo substituted benzo[b]thiophenes were synthesized starting from 2-alkynyl thioanisoles using a convenient electrophilic cyclization methodology that utilizes sodium halides as the source of electrophilic halogens when reacted along with copper(II) sulfate. This environmentally benign methodology is facile, uses ethanol as the solvent, and results in 3-halo substituted benzo[b]thiophene structures in very high yields. The cyclohexanol-substituted 3-chloro and 3-bromobenzo[b]thiophenes resulted in a low MIC of 16 µg/mL against Gram-positive bacteria and yeast. Additionally, in silico absorption, distribution, metabolism, and excretion (ADME) properties of the compounds were determined. The compounds with the lowest MIC values showed excellent drug-like properties with no violations to Lipinski, Veber, and Muegge filters. The time-kill curve was obtained for cyclohexanol-substituted 3-chlorobenzo[b]thiophenes against Staphylococcus aureus, which showed fast bactericidal activity at MIC.

ChemInform Abstract: Environmentally Benign Regio- and Stereoselective Synthesis of Functionalized Tertiary Amines.

ChemInform ◽  
2010 ◽  
Vol 41 (48) ◽  
pp. no-no
Author(s):  
Rendong Wang ◽  
Jian Li ◽  
Chunju Li ◽  
Jun Liu ◽  
Dafeng Li ◽  
...  
Keyword(s):  
Stereoselective Synthesis ◽  
Environmentally Benign ◽  
Tertiary Amines

scholarly journals Protein-engineering of an amine transaminase for the stereoselective synthesis of a pharmaceutically relevant bicyclic amine

2016 ◽  
Vol 14 (43) ◽  
pp. 10249-10254 ◽  
Author(s):  
Martin S. Weiß ◽  
Ioannis V. Pavlidis ◽  
Paul Spurr ◽  
Steven P. Hanlon ◽  
Beat Wirz ◽  
...  
Keyword(s):  
Transition Metal ◽  
Protein Engineering ◽  
Asymmetric Synthesis ◽  
Stereoselective Synthesis ◽  
Environmentally Benign ◽  
Attractive Alternative ◽  
P Application ◽  
Transition Metal Catalyzed ◽  
Prochiral Ketones ◽  
Metal Catalyzed

Application of amine transaminases (ATAs) for stereoselective amination of prochiral ketones represents an environmentally benign and economically attractive alternative to transition metal catalyzed asymmetric synthesis.

Environmentally Benign Regio- and Stereoselective Synthesis of Functionalized Tertiary Amines

2010 ◽  
Vol 28 (7) ◽  
pp. 1253-1256 ◽  
Author(s):  
Rendong Wang ◽  
Jian Li ◽  
Chunju Li ◽  
Jun Liu ◽  
Dafeng Li ◽  
...  
Keyword(s):  
Stereoselective Synthesis ◽  
Environmentally Benign ◽  
Tertiary Amines
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