52601-83-9Relevant academic research and scientific papers
New substituted spiro[cycloalkyl-1,3'-indo]-2'(1'H)-one derivatives and their use as p38 mitogen-activated kinase inhibitors
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Page/Page column 36, (2009/10/21)
This invention is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I) to processes for their preparation; to pharmaceutical compositions comprising them; and to their use in therapy.
Transition metal complexes with sulfur ligands, 135 [(+)] - Electron- rich Fe and Ru complexes with the new trisamine dithiolate ligand 'N3H3S2'-H2-bis(2-mercaptophenylamino)diethylamine]
Sellmann, Dieter,Utz, Jürgen,Heinemann, Frank W.
, p. 341 - 348 (2007/10/03)
In order to obtain iron and ruthenium complexes which are analogous to [M(L)('NHS4')] and [M(L)('N2H2S3')] complexes ['NHS4'2- = 2,2'-bis(2- mercaptophenylthio)diethylamine(2-), 'N2H2S3'2- = 2,2'-bis(2- mercaptophenylamino)diethylsulfide(2-)] but have electron-richer metal centers, the new pentadentate amine thiolate ligand 'N3H3S2'-H2 [ = 2,2'bis(2-mercaptophenylamino)diethylamine] (4) was synthesized. The dianion 'N3H3S2'2- reacted with Fe(II) salts to give high-spin [Fe('N3H3S2')] (5) [μ(eff) (293 K) = 3.94 μ(B)], which yielded diamagnetic [Fe(CO)('N3H3S2')] (6) upon reaction with CO. Complex 6 exhibits a low- frequency v(CO) band (1934 cm-1 in THF) indicating an electron-rich Fe center and a strong Fe-CO bond. In spite of this, 6 readily dissociated in solution to 5 and CO. The reaction of [RuCl2(PPh3)3] with 'N3H3S2'2- yielded [Ru(PPh3)('N3H3S2')] (7), which proved inert with respect to PPh3 substitution but could be methylated at the thiolate donors. The resulting [Ru(PPh3)('N3H3S2'-Me2)]I2 (8) proved as inert towards substitution as 7. Complex 8 could reversibly be deprotonated to give [Ru(PPh3)('N3'-H2S2'-Me2)]I (11), in the course of which the [RuPN3S2] cores rearrange from C(S) to C1 symmetry. Reversible protonation/deprotonation was also found with [Ru(NO)('N3'-H2S2')] (9) which formed from [RuCl3(NO)(PPh3)2] and 'N3H3S2'2- in the presence of one additional equivalent of LiOMe. Protonation of 9 with HBF4 gave [Ru(NO)('N3H3S2')]BF4 (10). The NMR spectra and the X-ray structure analysis of 8 proved that the [RuPN3S2] cores of 7 and 8 exhibit a Cs- symmetrical meso structure. In all other complexes, however, the [MLN3S2] cores exhibit a C1-symmetrical structure. It results from the fac-mer coordination mode of the 'N3H3S2'2- ligand and favors the planarization of amide donors when NH functions are reversibly deprotonated.
Enantiomers of 1-[(4-chlorophenyl)phenylmethyl]-4-[(4-methylphenyl) sulfonyl]piperazine
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, (2008/06/13)
Levorotatory and dextrorotatory enantiomers of 1-[(4-chlorophenyl)phenylmethyl]-4-[(4-methylphenyl)sulfonyl]piperazine of the formula STR1 their preparation and use for the preparation of substantially optically pure enantiomers of 1-[(4-chlorophenyl)phenylmethyl]piperazine, which are themselves valuable intermediate products for the preparation of optically active therapeutic compounds having a very high degree of optical purity.
Synthesis of Symmetrically Substituted Bicyclic Guanidines
Schmidtchen, Franz P.
, p. 2175 - 2182 (2007/10/02)
The symmetrically 2,2,8,8-tetraalkylsubstituted bicyclic guanidines 14a and b are prepared stereoselectively via construction of the open-chain triamines 11a and b and subsequent cyclisation.A one-pot reaction gives the unsubstituted guanidine 14c in high
