141492-50-4Relevant articles and documents
Discovery of indenopyrazoles as a new class of hypoxia inducible factor (HIF)-1 inhibitors
Minegishi, Hidemitsu,Fukashiro, Shinji,Ban, Hyun Seung,Nakamura, Hiroyuki
supporting information, p. 297 - 301 (2013/04/10)
The indenopyrazole framework was investigated as a new class of HIF-1α inhibitors. Indenopyrazole 2l was found to most strongly inhibit the hypoxia-induced HIF-1α transcriptional activity (IC50 = 0.014 μM) among all of the known compounds havin
New substituted derivatives of thiourea. Synthesis1H-NMR and IR spectra
Brǎtulescu, George
, p. 297 - 300 (2007/10/03)
Various new compounds of thiourea were synthesised by reaction of aromatic isothiocyanates with aminoesters. The 1H-NMR and IR spectra were interpreted.
New syntheses of aryl isothiocyanates
Besson, Thierry,Guillard, Jerome,Rees, Charles W.,Thiery, Valerie
, p. 889 - 892 (2007/10/03)
Primary aromatic amines are readily converted into arylimino-1,2,3-dithiazoles 2 and the derived cyanothioformanilides 6, both of which are rapidly cleaved by ethylmagnesium bromide in hot THF to give the corresponding isothiocyanates. The transformation 2→6→ArNCS can be performed as a 'one-pot' operation. The imines 2 are also converted, more slowly, into the isothiocyanates by sodium hydride in hot THF, via the cyanothioformanilides 6. Conversion of the anilides 6 into isothiocyanates is much faster under microwave irradiation in 2,6-lutidine. Mechanisms are proposed for these reactions.
New syntheses of aryl isothiocyanates from N-arylimino-1,2,3-dithiazoles
Besson, Thierry,Guillard, Jerome,Rees, Charles W.,Therisod, Michel
, p. 881 - 882 (2007/10/03)
Treatment of N-arylimino-1,2,3-dithiazoles 2 with ethylmagnesium bromide (2 equiv.) gives the corresponding aryl isothiocyanates 13, providing a very mild two-step conversion of ArNH2 into ArNCS avoiding hazardous reagents; alternatively the iminodithiazoles 2 can be converted into cyanothioformanilides 11 which rapidly give the same isothiocyanates with 1 equiv. of the Grignard reagent.
PIPERAZINYL DERIVATIVES AND METHODS OF TREATING CENTRAL NERVOUS SYSTEM AILMENTS RELATING TO THE 5-HT2 RECEPTOR SYSTEM
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, (2008/06/13)
Piperazinyl derivatives of the general formula I STR1 wherein R. sup.1 represents substituted phenyl, 1-or 2-diazanaphthyl, azadiazanaphtyl or diazanaphtyl groups; n is 1, 2, 3 or 4; X is--O--or STR2 wherein R. sup.2 is hydrogen, C 1-6-alkyl or C 3-8-cycloalkyl; Y is =O or =S or =NZ wherein Z is hydrogen, C. sub. 1-6-alkyl or--CN and R 3 is selected from a group consisting of various structures have been found to exhibit high affinity for various receptor subtypes including the 5-HT 2 receptor, the 5-HT 1A receptor, the alpha 1 receptor the dopamine receptor or a combination of these and may therefore be useful for treating CNS system, cardiovascular system and gastrointestinal disorders.