- HFIP-mediated strategy towards β-oxo amides and subsequent Friedel-Craft type cyclization to 2?quinolinones using recyclable catalyst
-
A simple and cost-effective 1,1,1,3,3,3-hexafluoro-2-propanol (HFIP)-mediated protocol for the synthesis of β-oxo amides has been described by using amines and β-keto esters as substrates. The reaction conditions were found to be highly efficient towards the cleavage of C[sbnd]O bond and consequent formation of the products in excellent yields and selectivity. The obtained β-oxo amides were further transformed in to the synthetically useful 2?quinolinones via intramolecular Friedel-Craft type cyclization of aromatic ring using ferrites as a recyclable catalyst. A spectrum of substrates bearing broad range of functional groups were well tolerated under the reaction conditions. The proposed mechanistic pathways were substantially verified by literature and mass-spectroscopic evidences.
- Kabi, Arup K.,Gujjarappa, Raghuram,Vodnala, Nagaraju,Kaldhi, Dhananjaya,Tyagi, Ujjawal,Mukherjee, Kalisadhan,Malakar, Chandi C.
-
supporting information
(2020/10/20)
-
- Synthesis and biological evaluation of a novel class as antileishmanial agent
-
Leishmaniases are a group of diseases caused by the protozoan parasites of the genus Leishmania. Despite the tremendous progress made in the understanding of the biochemistry and molecular biology of the parasite, the first choice treatment for leishmaniases still relies on pentavalent antimonial developed more than 50 years ago. These drugs are potentially toxic and often ineffective. The spread of drug resistance, combined with other shortcoming of the available antileishmanial drugs, emphasizes the importance of developing new effective, and safe drugs against leishmaniasis. The study reported here was undertaken to examine the antileishmanial activity of novel substituted 1,2,3,4- tetrahydropyrimidine-5-carboxamide (I) or cabohydrazide (II) analogs both in vivo and in vitro against Leishmania major. All tested compounds showed in vitro antileishmanial activity, but only four compounds showed in vivo activity in Swiss strain albino mice model as revealed by clinical cure of the cutaneous lesion, parasitologically by marked reduction in parasitic load and by histopathological changes. Springer Science+Business Media, LLC 2010.
- Saudi,El-Semary,Elbayaa,Jaeda,Eissa,Amer,Baddour
-
experimental part
p. 257 - 267
(2012/09/05)
-