344951-08-2Relevant articles and documents
Carbazole compounds and therapeutic uses of the compounds
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, (2015/09/28)
Compounds of the general structural formula (I) and (II) and use of the compounds and salts and hydrates thereof, as therapeutic agents are disclosed. Treatable diseases and conditions include cancers, inflammatory diseases and conditions, and immunodeficiency diseases. (I), (II).
Intramolecular Pd(II)-catalyzed aerobic oxidative amination of alkenes: Synthesis of six-membered N-heterocycles
Lu, Zhan,Stahl, Shannon S.
supporting information; experimental part, p. 1234 - 1237 (2012/04/18)
Use of a base-free Pd(DMSO)2(TFA)2 catalyst system enables the synthesis of six-membered nitrogen heterocycles via a Wacker-type aerobic oxidative cyclization of alkenes bearing tethered sulfonamides. Various heterocycles, including morpholines, piperidines, piperazines, and piperazinones, are accessible by this method.
Development of hypoxia-sensitive Gd3+-based MRI contrast agents
Iwaki, Shimpei,Hanaoka, Kenjiro,Piao, Wen,Komatsu, Toru,Ueno, Tasuku,Terai, Takuya,Nagano, Tetsuo
, p. 2798 - 2802 (2012/06/01)
Hypoxia occurs in various diseases, including cancer, ischemia, and acute and chronic vascular diseases. Here we describe the design and synthesis of the first hypoxia-sensitive MRI contrast agents, SAGds. SAGds showed a pH-dependent r1 relaxivity change associated with intramolecular chelation of the nitrogen atom of the sulfonamide moiety to the Gd3+ center. There was a correlation between the pKa of the r1 relaxivity change and the sum of the Hammett σ constants of substituents on the aromatic ring. Among the synthesized compounds, 4NO22MeOSAGd was selectively reduced to the amine by rat liver microsomes under hypoxic conditions, resulting in a 1.8-fold increment of the r1 relaxivity owing to the change in pKa of the arylsulfonamide moiety. This enhancement of the r 1 relaxivity could be clearly detected in T1-weighted MR images. Thus, 4NO22MeOSAGd is a 'smart' MRI contrast agent for the detection of hypoxia under physiological conditions.
Methods of making 2,6-diaryl piperidine derivatives
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, (2008/06/13)
Methods for preparing 2,6-diaryl piperidine derivatives are described. More particularly, 2,6-diaryl piperidines having formula 1-4 are prepared by cyclocondensation of an aryl or heteroaryl aldehyde with 1,3-acetonedicarboxylic acid.
Chiral peptide nucleic acids with a n-aminoethyl-d-proline backbone
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, (2008/06/13)
Chiral peptide nucleic acids are provided which hybridise strongly with complementary nucleic acids and have potential as antigene and antisense agents and as tools in molecular biology. The compounds have the formulae: where n is 1 to 200, B is a protect
Facile synthesis of a selectively protected triazamacrocycle
Skerlj, Renato T.,Nan, Siqiao,Zhou, Yuanxi,Bridger, Gary J.
, p. 7569 - 7571 (2007/10/03)
1,7-Diaminoheptane was selectively homologated with the novel reagent N-(2-nitrobenzenesulfonyl)aziridine. A series of reactions then followed to afford a selectively protected 14-membered triazamacrocyclic ring.
