Efficient synthesis of unsymmetrical heteroaryl thioethers and chalcogenides by alkali hydroxide-mediated SNAr reactions of heteroaryl halides and dichalcogenides

RSC Advances ◽  
2016 ◽  
Vol 6 (62) ◽  
pp. 56930-56935 ◽  
Author(s):  
Xiantao Ma ◽  
Quan Liu ◽  
Xiaojuan Jia ◽  
Chenliang Su ◽  
Qing Xu
Keyword(s):  
Efficient Synthesis ◽  
Practical Synthesis ◽  
Alkali Hydroxide

An efficient SNAr reaction of heteroaryl halides and diorganyl dichalcogenides is developed for practical synthesis of the useful unsymmetrical heteroaryl thioethers and chalcogenides.

Efficient Synthesis of a 5α-Reductase Inhibitor, 3-(Tetrazol-5-yl)-3,5-pregnadien-20-one through Allylic Rearrangement of Cyanophosphates

Synthesis ◽  
2019 ◽  
Vol 51 (08) ◽  
pp. 1791-1794 ◽  
Author(s):  
Hiroki Yoneyama ◽  
Yoshihide Usami ◽  
Shinya Harusawa
Keyword(s):  
Reductase Inhibitor ◽  
Allylic Rearrangement ◽  
Efficient Synthesis ◽  
Practical Synthesis

We describe the use of allylic rearrangements of cyanophosphates for the efficient and practical synthesis of 3-(tetrazol-5-yl)-3,5-pregnadien-20-one, which is a potent 5α-reductase inhibitor (IC50: 15.6 nM), from pregnene-3,20-dione in 92% overall yield in four steps.

scholarly journals Zeolite catalyzed solvent-free one-pot synthesis of dihydropyrimidin-2(1H)-ones – A practical synthesis of monastrol

2009 ◽  
Vol 5 ◽  
Author(s):  
Mukund G Kulkarni ◽  
Sanjay W Chavhan ◽  
Mahadev P Shinde ◽  
Dnyaneshwar D Gaikwad ◽  
Ajit S Borhade ◽  
...  
Keyword(s):  
Potent Inhibitor ◽  
Cost Effective ◽  
Solvent Free ◽  
Environmentally Benign ◽  
Efficient Synthesis ◽  
One Pot ◽  
One Pot Synthesis ◽  
Benign Process ◽  
Practical Synthesis ◽  
Kinesin Eg5

A zeolite-catalyzed, simple, one-pot, solvent-free, cost effective, and environmentally benign process for the synthesis of dihydropyrimidones is described. This reaction is scaleable to multigram scale and the catalyst is recyclable. This methodology has resulted in an efficient synthesis of monastrol, a potent inhibitor of kinesin Eg5.

A practical and efficient route to heteraphanes: synthesis of structurally simplified analogues of ansamycins

RSC Advances ◽  
2016 ◽  
Vol 6 (72) ◽  
pp. 68199-68203 ◽  
Author(s):  
R. Santhosh Reddy ◽  
Shaojun Zheng ◽  
Chandraiah Lagishetti ◽  
Hengyao You ◽  
Yun He
Keyword(s):  
Mitsunobu Reaction ◽  
Efficient Synthesis ◽  
Diverse Range ◽  
Mild Conditions ◽  
Efficient Route ◽  
Practical Synthesis

The intramolecular Mitsunobu reaction has been employed for the practical synthesis of a wide variety of heteraphanes. This strategy enabled the efficient synthesis of a diverse range of macrocycles with varying ring sizes under mild conditions.

An efficient synthesis of 2,4,7-trisubstituted pyrimido[1,2-a][1,3,5]triazin-6-ones

2015 ◽  
Vol 39 (6) ◽  
pp. 4796-4804 ◽  
Author(s):  
Nikhil Sachdeva ◽  
Anton V. Dolzhenko ◽  
Seow Joo Lim ◽  
Wee Ling Ong ◽  
Wai Keung Chui
Keyword(s):  
Biological Activity ◽  
Efficient Synthesis ◽  
Practical Synthesis ◽  
Theoretical Assessment

A practical synthesis of 3,4-dihydro pyrimido[1,2-a][1,3,5]triazin-6-ones, experimental and theoretical assessment of their tautomeric preferences and biological activity results are presented.

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