134810-89-2Relevant academic research and scientific papers
Enantioselective Synthesis of trans-2,3-Dihydro-1H-indoles Through C–H Insertion of α-Diazocarbonyl Compounds
Santi, Micol,Müller, Simon T. R.,Folgueiras-Amador, Ana A.,Uttry, Alexander,Hellier, Paul,Wirth, Thomas
, p. 1889 - 1893 (2017)
A stereoselective synthesis of 2,3-dihydro-1H-indoles with a RhII-catalyzed C–H insertion is reported. The α-diazo carbonyl intermediates can be obtained by a diazo-transfer reaction of 2-aminophenylacetic acids. Optimization and kinetic studie
Ti/Ni-mediated inter- and intramolecular conjugate addition of aryl and alkenyl halides and triflates
Marquez, Irene R.,Miguel, Delia,Millan, Alba,Marcos, M. Luisa,De Cienfuegos, Luis Alvarez,Campana, Araceli G.,Cuerva, Juan M.
, p. 1529 - 1541 (2014/03/21)
In this work, we show that the unique combination of a nickel catalyst and Cp2TiCl allows the direct conjugate addition of aryl and alkenyl iodides, bromides, and to a lesser extent, chlorides and triflates to α,β-unsaturated carbonyls at room temperature, without requiring the previous formation of an organometallic nucleophile. The reaction proceeds inter- and intramolecularly with good functional group compatibility, which is key for the development of free protecting group methodologies. Carbo- and heterocycles of five- and six-membered rings are obtained in good yields. Moreover, some insights about the mechanism involved have been obtained from cyclic voltammetry, UV-vis, and HRTEM measurements.
VLA-4 INHIBITORS
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, (2008/06/13)
The present invention relates to a compound represented by the following formula (I): (wherein, W represents WA-A1 -WB - (in which, WA is substituted or unsubstituted aryl, etc., A1 is -NR1-, single bond, -C(O)-, etc., and WB is substituted or unsubstituted arylene, etc.), R is single bond, -NH-, -OCH2-, alkenylene, etc., X is -C(O) -CH2-, etc., and M is, for example, the following formula: (in which, R11, R12 and R13 each independently represents hydrogen, hydroxyl, amino, halogen, etc., R14 is hydrogen or lower alkyl, Y represents -CH2-O-, etc., Z is substituted or unsubstituted arylene, etc., A2 is single bond, etc, and R10 is hydroxyl or lower alkoxy)), or salt thereof; and a medicament containing the same. This compound or salt thereof selectively inhibits binding of cell adhesion molecules to VAL-4 and exhibits high bioavailability so that it is useful as a preventive and/or remedy for inflammatory diseases, autoimmune diseases, metastasis, bronchial asthma, rhinostenosis, diabetes, and the like.
Practical synthesis of 1H-indazole-3-carboxylic acid and its derivatives
Yoshida, Toyokichi,Matsuura, Noriyasu,Yamamoto, Katsuhisa,Doi, Masahiro,Shimada, Kanji,Morie, Toshiya,Kato, Shiro
, p. 2701 - 2712 (2007/10/03)
A practical and convenient synthesis of 1H-indazole-3-carboxylic acid and its amide and ester derivatives from the corresponding derivatives of 2-nitrophenylacetic acid was described.
Anionic hetero[3,3] and [3,5][ rearrangements of hydroxylamine derivatives accompanied with N-O bond cleavage
Endo,Uchida,Hizatate,Shudo
, p. 1096 - 1105 (2007/10/02)
Aromatic and aliphatic N,O-divinylhydroxylamine systems generated in situ from hydroxylamine derivatives smoothly undergo [3,3] rearrangement. The base-catalyzed formation and rearrangement of enolates or dienolates of N-aryl-O-acylhydroxylamines, N,O-dia
Anionic [3,3]-sigmatropic rearrangement of N-phenyl-O-acylhydroxylamines to o-aminophenylcetic acids
Endo, Yasuyuki,Hizatate, Shoji,Shudo, Koichi
, p. 2803 - 2806 (2007/10/02)
N-Phenyl-O-acylhydroxylamines rearrange under basic conditions to afford o-aminophenylacetic acids. The rearrangement can be rationalized in terms of [3,3]-sigmatropic shifts of an enolized N-phenyl-O-acylhydroxyl-amine.
