- Silica-supported boric acid catalyzed synthesis of dihydropyrimidin-2-ones, bis(indolyl)methanes, esters and amides
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Silica-supported boric acid (H3BO3-SiO2) has been established as a green, efficient and recyclable catalyst for the synthesis of dihydropyrimidin-2-ones, bis(indolyl)methanes, and acetylation of alcohols, phenols, amines and thiols under solvent free conditions. The main features of the present method include clean reaction, mild conditions, low loading of environment friendly catalyst and easy workup procedure. The catalyst can be recycled at least five times without any significant loss in activity.
- Kumar, Vishal,Singh, Chitra,Sharma, Upendra,Verma, Praveen K.,Singh, Bikram,Kumar, Neeraj
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- An expedient synthesis of novel 2-substituted thiazolo[4,5-f]isoquinolines/ quinolines and benzo[1,2-d:4,3-d']bisthiazoles and their potential as inhibitors of COX-1 and COX-2
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An efficient, general synthesis of 2-substituted thiazolo[4,5-f] isoquinolines, thiazolo[4,5-f]-quinolines and benzo[1,2-d:4,3-d']bisthiazoles has been accomplished from 5-nitroisoquinoline/quinoline and 6-nitrobenzothiazole, respectively, and all the products have been thoroughly identified spectroscopically (IR, 1H and 13C NMR, LR/HR EI/FAB/ESI-MS). The synthesis of thiazolo[4,5-f]isoquinolines constitutes the first synthesis of this class of heteroarenes. Eighteen compounds, covering all three types, were screened for inhibition of COX-1 and COX-2, and some of them showed moderate activities. ARKAT-USA, Inc.
- Chakrabarty, Manas,Mukherji, Ajanta,Karmakar, Sulakshana,Mukherjee, Ratna,Nagai, Kenichiro,Geronikaki, Athina,Elenic, Pitta
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experimental part
p. 265 - 290
(2011/02/24)
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