102422-37-7Relevant academic research and scientific papers
Synthesis, characterization, and biological evaluations of substituted phenethylamine-based urea as anticancer and antioxidant agents
?zgeri?, Fatma Betül,?zgeri?, Bünyamin
, p. 1241 - 1250 (2021)
Cancer is one of the most important diseases. It is the second leading cause of death worldwide following cardiovascular disease. There is a need to develop new chemotherapeutic agents for the treatment of cancer and it is still a significant task for med
Process for the Preparation of Solifenacin and Salts Thereof
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Paragraph 0076-0078, (2014/08/19)
The invention provides a new process for the preparation of solifenacin or a pharmaceutically acceptable acid addition salt thereof, comprising reacting (R)-quinuclidin-3-yl phenethylcarbamate with benzaldehyde in the presence of an acid to obtain a diast
PROCESS FOR THE PREPARATION OF SOLIFENACIN AND SALTS THEREOF
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Page/Page column 18, (2013/02/28)
The invention provides a new process for the preparation of solifenacin or a pharmaceutically acceptable acid addition salt thereof, comprising reacting (R)- quinuclidin-3-yl phenethylcarbamate with benzaldehyde in the presence of an acid to obtain a diasteroisomeric mixture (S,R)-((R)-quinuclidin-3-yl) 1 -phenyl-3,4- dihydroisoquinoline-2(1 H)-carboxylate of formula (IV) which can be resolved and the solifenacin or a pharmaceutically acceptable acid addition salt thereof recovered. The invention also provides the new key intermediate (R)-quinuclidin-3-yl phenethylcarbamate involved in the process. Further the invention provides a method for the transformation of (R)-((R)-quinuclidin-3-yl) 1 -phenyl-3,4- dihydroisoquinoline-2(1 H)-carboxylate into a diasteroisomeric mixture (S,R)-((R)- quinuclidin-3-yl) 1 -phenyl-3,4-dihydroisoquinoline-2(1 H)-carboxylate.
COMPOUNDS FOR THE TREATMENT OF DISEASES
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Page/Page column 66, (2008/06/13)
The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in
The 4-azidobenzyloxycarbonyl function; application as a novel protecting group and potential prodrug modification for amines
Griffin, Roger J.,Evers, Elaine,Davison, Richard,Gibson, Ashleigh E.,Layton, Deborah,Irwin, William J.
, p. 1205 - 1211 (2007/10/03)
A series of 4-azidobenzylcarbamates [4-N3-C6H4-CH2-O-CO-N(H)-C 6H4-X; X = H, Me, MeO, Br, Cl, NO2] have been prepared in good yield, and in high purity, by reaction of 4-azidobenzyl alcohol with the corresponding aryl isocyanate, or by displacement of 4-nitrophenol from 4-azidobenzyl-4-nitrophenylcarbonate by the appropriate amine. The 4-azidobenzylcarbamates were shown to undergo rapid reduction in the presence of dithiothreitol, and the resultant 4-aminobenzylcarbamates underwent immediate cascade degradation to release the target amine. The mild conditions used in this conversion may prove useful in the protection of amines during synthetic procedures or as a possible mode of bioactivation of prodrugs.
Inactivation of Leukocyte Elastase by Aryl Azolides and Sulfonate Salts. Structure-Activity Relationship Studies
Groutas, W. C.,Brubaker, M. J.,Zandler, M. E.,Mazo-Gray, V.,Rude, S. A.,et al.
, p. 1302 - 1305 (2007/10/02)
The inhibitory activity of a series of aryl azolides and sulfonate salts toward human leukocyte elastase is reported.Several of the compounds were found to be potent inhibitors of the enzyme.Active compounds were obtained only when the specificity group and the reactive moiety were separated by a two-carbon chain.The introduction of hydrophobic groups enhanced the inhibitory activity of these compounds, with the exception of the sulfonate salts.The nature of the leaving group had had a profound effect on inhibitory activity, with compounds 23 and 26 being the most active (kobsd/ = 11722 and 13500 M-1 s-1, respectively).
