Synthesis of Novel 2-diethylamino-4H-7-(Het) aryl pyrido[1,2-a][1,3,5]triazin-4-ones via a Suzuki Cross-Coupling Reaction of 2-Diethylamino-4H-7-iodopyrido[1,2a][1,3,5]triazin-4-one with (Het) arylboronic Acids in Water

2021 ◽  
Vol 12 (3) ◽  
pp. 563-572
Author(s):  
Said Dagdag ◽  
Mounir Belbahloul ◽  
Maria Kopp ◽  
Abdellah Anouar ◽  
Moustafa Chhiba ◽  
...  

Suzuki cross coupling reaction is one of the most famous organic reactions of the 20th century’s chemistry. It is deemed of as one of the most famous reaction in the field of chemistry. It is a very effective method for making carbon–carbon bonds. It has been extensively utilized in the synthesis of many carbon molecules including the most complex ones.Syntheses of 2-diethylamino-4H-7-(Het) aryl pyrido [1,2-a] [1,3,5] triazin-4-ones are currently under investigation in order to obtain great potentialities in medicinal chemistry of compounds class. The methodology we propose herein is able to produce numerous 2-diethylamino-4H-7-(Het)arylpyrido[1,2-a][1,3,5]triazin-4-one and derivatives that were synthesized, purified and characterized by 1HNMR, 13CNMR, MS techniques. Furthermore, it allows sequential introduction of various substituents into a 2-alkylylamino-4H-7-(Het)arylpyrido[1,2-a][1,3,5]triazin-4-ones ring using a one-pot procedure. The biological evaluation as well as the physico-chemical characterisation of various products are currently under way and will be described elsewhere.

2010 ◽  
Vol 17 (2) ◽  
pp. 440-444 ◽  
Author(s):  
Weiguo Huang ◽  
Ming Wang ◽  
Chun Du ◽  
Yulan Chen ◽  
Ruiping Qin ◽  
...  

RSC Advances ◽  
2018 ◽  
Vol 8 (70) ◽  
pp. 40000-40015 ◽  
Author(s):  
Nedra Touj ◽  
Abdullah S. Al-Ayed ◽  
Mathieu Sauthier ◽  
Lamjed Mansour ◽  
Abdel Halim Harrath ◽  
...  

The in situ prepared four component system Pd(OAc)2, 1,3-dialkylbenzimidazolium halides 2a–i and 4a–i, K2CO3 under CO atmosphere catalyses carbonylative cross-coupling reaction of 2-bromopyridine with various boronic acids to yield unsymmetrical arylpyridine ketones.


2014 ◽  
Vol 43 (13) ◽  
pp. 5014-5020 ◽  
Author(s):  
Algin Oh Biying ◽  
Venu R. Vangala ◽  
Chia Sze Chen ◽  
Ludger Paul Stubs ◽  
Narayan S. Hosmane ◽  
...  

Author(s):  
Jonathon Moir

Pharmaceuticals and drugs have become an indispensable part of human life. Presently, a myriad of different drugs are available for a variety of mental and physical health concersn. The synthesis of these drugs, however, remains an elusive and often difficult aspect of the industry. The importance of chirality, or "handedness", in the synthesis of natural products is paramount, as any given pair of enantiomers can have widely differing physiological effects. As such, the ability to control the enantioselectivity of a reaction is of the utmost importance. One example of a facile method used to form carbon-carbon bonds is the Suzuki-Miyaura cross-coupling reaction. Not only is this reaction effective at coupling primary organoboronic esters with organohalides, but recent work in the Crudden group in the Department of Chemistry has revealed an effective method of also cross-couplingchiral secondary organoboronic esters with good retention of stereochemistry. This work, the first of its kind, is crucial in developing single-handed natural products for a wide array of applications, including applications in the pharmaceutical industry. The end result is safer and more effective drugs for distribution to the general public. To expand the scope of this project, new substrates are currently being synthesized for cross-coupling applications. The overall goal is to improve upon current methodologies, while helping to meet the industrial and academic needs of the future.  


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