Superacidic Cyclization of Activated Anthranilonitriles into 2-Unsubstituted-4-aminoquinolines
4-Aminoquinolines were prepared in a three-step synthesis starting from substituted anthranilonitriles. The condensation on 1,1,1-trichloro-4-ethoxybut-3-enone proceeded efficiently either neat or in refluxing EtOH. Cyclization in superacidic trifluoromethanesulfonic acid provided unstable intermediate, which upon treatment with NaOEt in ethanol, afforded the expected esters. Theoretical investigations pointed out a monoprotonated nitrilium as the reactive species during the cyclization process.
Lavrard, Hubert,Larini, Paolo,Popowycz, Florence
p. 4203 - 4206
(2017/08/23)
HETEROCYCLIC DERIVATIVES FOR TREATMENT OF HYPERLIPIDEMIA AND RELATED DISEASES
The present invention provides compositions adapted to enhance reverse cholesterol transport in mammals. The compositions are suitable for oral delivery and useful in the treatment and/or prevention of hypercholesterolemia, atherosclerosis and associated
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Page/Page column 88-89
(2010/02/15)
A new [5+1]-annulation route to some quinazoline and fused pyrimidine derivatives
β-Dicarbonyl compounds, such as diethyl malonate, ethyl acetoacetate and acetyl acetone have been found to add selectively to the iminoether functionality of the 2-ethoxymethyleneaminonitriles leading to a one-pot synthesis of some quinazoline and fused p
Chattopadhyay, Shital K.,Dey, Rajat,Biswas, Suman
p. 1083 - 1086
(2007/10/03)
Synthesis of 4-substituted aminoquinoline-3-carboxylates as potential antimicrobial agents
A series of 4-substituted aminoquinoline-3-carboxylates was prepared and evaluated for antimicrobial activity. Four of the compounds (VIII, XIII, XV, and XXIII) exhibited low activity against Staphylococcus aureus.
Marecki,Bambury
p. 1141 - 1143
(2007/10/02)
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