213771-94-9Relevant academic research and scientific papers
Synthesis of acylsilanes by palladium-catalyzed cross-coupling reaction of thiol esters and silylzinc chlorides
Azuma, Hiroki,Okano, Kentaro,Tokuyama, Hidetoshi
, p. 959 - 961 (2011/12/05)
An acylsilane synthesis by a Pd-catalyzed cross-coupling reaction of thiol esters and silylzinc chlorides was developed. S-Phenyl thiol esters with a variety of functional groups were converted to corresponding acylsilanes.
Intramolecular aldol reaction of N-Acylated (2-Aminophenyl)-α- oxoacetic Acids: Rapid access to Tri- and tetracyclic 1,2-dihydroquinolin-2(1 H)-ones
Hellal, Malik,Cuny, Gregory D.
supporting information; experimental part, p. 3465 - 3468 (2010/08/07)
A four-step synthesis of tri- and tetracyclic 1,2-dihydroquinolin-2(1H)- ones via acylation of various substituted isatins with readily available N-Boc-protected aminoacids followed by an intramolecular aldol reaction and cyclization has been developed. The final products were obtained in moderate to excellent overall yields.
Pyrimidinone-1,3-oxathiolane derivatives with antiviral activity
-
, (2008/06/13)
Compounds of formula (I) wherein Ra and Rb the same or different, are hydrogen atoms, acyl groups deriving from a lower carboxylic acid or chains of formula (a) useful as reverse transcriptase inhibitors antiviral activity are described.
New anti-HIV derivatives: Synthesis and antiviral evaluation
De Michelis,Rocheblave,Priem,Chermann,Kraus
, p. 1253 - 1262 (2007/10/03)
A small focused library of 18 compounds incorporating the motif 1,3-(N,N'-dibenzyl)diamino-2-propanol has been synthesized, using adapted synthetic methodologies. These series of compounds were evaluated for their in vitro anti-HIV activity on infected MT4 cells (syncytium formation observation). Some of the new synthesized compounds show potent anti-HIV activities. EC50 values for compounds (31, 40, 34, 37 and 46Scheme 3(i) Na2SO4, CH2Cl2, rt; (ii) NaBH4, EtOH, 0°C; (iii) Boc2O, CH2Cl2, 0°C; (iv) DMSO, TFAA, Et3N, CH2Cl2, -60°C; (v) TFA, CH2Cl2, rt; (vi) BOP, RCOOH, Et3N, CH2Cl2, rt.) range from 0.1 to 1μM. In order to determine at which level these new derivatives interfere with the HIV replicative cycle, inhibition assays on recombinant HIV protease and HIV integrase have been performed. None of the compounds were found active on these two enzymatic targets. Experiments are in progress in order to identify their biological target within the HIV replicative cycle. Copyright (C) 2000 Elsevier Science Ltd.
