698-19-1Relevant academic research and scientific papers
Multi-substituted amine compound and its preparation and use (by machine translation)
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Paragraph 0208; 0507; 0509; 0511; 0512, (2018/04/27)
The invention belongs to the field of medical technology, in particular, the present invention provides the following formula I shown multi-substituted amine compound or its isomer or its pharmaceutically acceptable salt, ester, prodrug or hydrate, its pharmaceutical composition, preparation method thereof and its use in the preparation of medicine for treating aids in use. The compound or pharmaceutical composition containing the compound can be used as an inhibitor for inhibiting HIV integrase with LEDGF/p75 between protein - protein interaction and HIV integrase dimerization, then can be used for the treatment of aids. . (by machine translation)
Selective monomethylation of primary amines with simple electrophiles
Lebleu, Thomas,Ma, Xiaolu,Maddaluno, Jacques,Legros, Julien
supporting information, p. 1836 - 1838 (2014/02/14)
Direct monomethylation of primary amines with methyl triflate was achieved with high selectivity (up to 96%). The key point of this single methyl transfer stems from the use of HFIP as the solvent that interferes with amines and avoids overmethylation.
Highly enantioselective organocatalytic trifluoromethyl carbinol synthesis-a caveat on reaction times and product isolation
Duangdee, Nongnaphat,Harnying, Wacharee,Rulli, Giuseppe,Neudoerfl, Joerg-M.,Groeger, Harald,Berkessel, Albrecht
experimental part, p. 11196 - 11205 (2012/08/28)
Aldol reactions with trifluoroacetophenones as acceptors yield chiral α-aryl, α-trifluoromethyl tertiary alcohols, valuable intermediates in organic synthesis. Of the various organocatalysts examined, Singh's catalyst [(2S)-N-[(1S)-1-hydroxydiphenylmethyl
A simple efficient sequential one-pot intermolecular aza-Michael addition and intramolecular Buchwald-Hartwig α-arylation of amines: Synthesis of functionalized tetrahydroisoquinolines
Reddy, Alavala Gopi Krishna,Satyanarayana, Gedu
scheme or table, p. 8003 - 8010 (2012/09/25)
An efficient one-pot sequential intermolecular aza-Michael addition and Pd-catalyzed intramolecular Buchwald-Hartwig α-arylation of secondary amines have been investigated, for the synthesis of tetrahydroisoquinolines. This method is simple and furnished
Synthesis and antitumor evaluation of a novel class of 4-substituted-1,4- dihydroisoquinolin-3-ones
Ma, Ting,Chen, Wenteng,Zhang, Guolin,Yu, Yongping
scheme or table, p. 488 - 490 (2010/09/05)
An efficient method for the solution-phase parallel synthesis of 4-substituted-1,4-dihydroisoquinolin-3-ones is developed. The isoquinolinones were constructed employing an intramolecular Heck reaction, providing full regio- and stereoselectivity. Most of
Antimycobacterial activity of new 3,5-disubstituted 1,3,4-oxadiazol-2(3H)-one derivatives. Molecular modeling investigations
Zampieri, Daniele,Mamolo, Maria Grazia,Laurini, Erik,Fermeglia, Maurizio,Posocco, Paola,Pricl, Sabrina,Banfi, Elena,Scialino, Giuditta,Vio, Luciano
experimental part, p. 4693 - 4707 (2009/10/24)
3H-1,3,4-Oxadiazol-2-one derivatives were synthesized and tested for their in vitro antimycobacterial activity. Oxadiazolone derivatives showed an interesting antimycobacterial activity against the reference strain of Mycobacterium tuberculosis H37Rv. Molecular modeling investigations were performed and showed that the active compounds possess all necessary features to target the protein active site of the mycobacterial cytochrome P450-dependent sterol 14α-demethylase in the sterol biosynthesis pathway as the calculated free energy of binding were in agreement with the corresponding MIC values.
TACHYKININ RECEPTOR ANTAGONISTS
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Page 29, (2010/02/10)
The present invention relates to selective NK-1 receptor antagonists of Formula (I) or a pharmaceutically acceptable salt thereof, for the treatment of disorders associated with an excess of tachykinins.
USE OF COMPOUNDS HAVING AN AMINE NUCLEUS IN MANUFACTURE OF A MEDICAMENT USEFUL FOR TREATING FACTOR VIIA-ASSOCIATED CONDITIONS
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Page 38, (2008/06/13)
Use of at least one compound having the formula (I), or a pharmaceutically-acceptable salt, hydrate or prodrug thereof, in the manufacture of a medicament useful for treating conditions associated with the activity of Factor VIIa is described.
UREIDO-SUBSTITUTED ANILINE COMPOUNDS USEFUL AS SERINE PROTEASE INHIBITORS
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Page 38, (2008/06/13)
Compounds having formula (I), or pharmaceutically-acceptable salts, hydrates or prodrugs thereof, are effective as inhibitors of Factor VIIa.
Highly stereoselective Friedel-Crafts type cyclization. Facile access to enantiopure 1,4-dihydro-4-phenyl isoquinolinones
Philippe, Nicolas,Denivet, Fran?ois,Vasse, Jean-Luc,Sopkova-De Olivera Santos, Jana,Levacher, Vincent,Dupas, Georges
, p. 8049 - 8056 (2007/10/03)
The present report describes a stereoselective synthesis of 1,4-dihydro-4-phenyl isoquinolinones 5 based on a stereoselective Friedel-Crafts type cyclization. Cyclization precursors 1 were prepared in two steps, from the readily available (S)-mandelic acid, in 60-80% overall yield. The stereoselective electrophilic cyclization was accomplished in 20-86% yield and with 20-97% ee. In the course of this work, the presence of the amide carbonyl was found to be particularly important to guarantee a stereospecific process during the electrophilic aromatic substitution.
