N-Alkylation of poor nucleophilic amines and derivatives with alcohols by a hydrogen autotransfer process catalyzed by copper(II) acetate: scope and mechanistic considerations
作者:Ana Martínez-Asencio、Diego J. Ramón、Miguel Yus
DOI:10.1016/j.tet.2011.02.075
日期:2011.4
simple catalyst for the selective N-monoalkylation of amino derivatives with poor nucleophilic character, such as aromatic and heteroaromatic amines as well as carboxamides, phosphinamides, sulfonamides, and phosphazenes, using in all cases primary alcohols as initial source of the electrophiles, through a hydrogen autotransfer process. In the case of sulfonamides, the monoalkylation process followed
[EN] TRICYCLIC AMINO CONTAINING COMPOUNDS FOR TREATMENT OR PREVENTION OF SYMPTOMS ASSOCIATED WITH ENDOCRINE DYSFUNCTION<br/>[FR] COMPOSÉS CONTENANT DES ACIDES AMINÉS TRICYCLIQUES POUR LE TRAITEMENT OU LA PRÉVENTION DE SYMPTÔMES ASSOCIÉS À UN DYSFONCTIONNEMENT ENDOCRINIEN
申请人:UNIV EMORY
公开号:WO2013070660A1
公开(公告)日:2013-05-16
The disclosure provides methods of use of certain compounds that are useful for treating certain symptoms of endocrine disturbances, and in particular those associated with hot flashes.
本公开提供了使用某些化合物治疗内分泌紊乱的某些症状的方法,特别是与潮热相关的症状的方法。
Syntheses and structures of copper(i) complexes based on CunXn (X = Br and I; n = 1, 2 and 4) units and bis(pyridyl) ligands with longer flexible spacer
Structural analyses show that the eight complexes possess an increasing dimensionality from 0D (1–3) to 1D (4) to 2D (5–8), in which 1 and 2 contain a CuX unit, 2–7 contain a Cu2X2 unit and 8 contains a Cu4X4 unit. Such evolvement indicates that the conformation of flexible bis(pyridyl) ligands and the participation of triphenylphosphine (PPh3) as a second ligand take an essential role in the framework
自组装四 双(吡啶基) 具有更长的柔性间隔基的配体: 1,4-双(3-吡啶基氨基甲基)苯(L1),1,4-双(2-吡啶基氨基甲基)苯(L2),1,3-双(3-吡啶基氨基甲基)苯(L3)和1,3-双(2-吡啶基氨基甲基)苯(L4),以及铜 (X = 溴和I)导致形成八个基于[Cu n X n ]的(X =溴和我; n = 1、2和4)配合物[Cu 2 I 2 L1(PPh 3)4 ](1),[Cu 4 Cl 2 Br 2(L4)2(PPh 3)6 ]·(CH 3 CN)2(2),[Cu 2 I 2(L3)2 ](3),[Cu 2 Br 2 L2(PPh 3)2 ]·(CH 2 Cl 2)2 } n( 4),[CuI L1 ] n ·nCH 2 Cl 2( 5),[CuI L1 ] n( 6),[CuI L4 ] n( 7)和[Cu 2 I 2 L4 ] n( 8) ,已通过元素分析,IR,
Tricyclic amino containing compounds for treatment or prevention of symptoms associated with endocrine dysfunction
申请人:Emory University
公开号:US10632120B2
公开(公告)日:2020-04-28
The disclosure provides methods of use of certain compounds that are useful for treating certain symptoms of endocrine disturbances, and in particular those associated with hot flashes.
Metal-Free Catalysts for the Hydrolysis of RNA Derived from Guanidines, 2-Aminopyridines, and 2-Aminobenzimidazoles
作者:Ute Scheffer、Andreas Strick、Verena Ludwig、Sascha Peter、Elisabeth Kalden、Michael W. Göbel
DOI:10.1021/ja0443934
日期:2005.2.1
2-Aminopyridine and 2-aminobenzimidazole were chosen as structural analogues to substitute guanidinium groups in receptor molecules designed as phosphoryl transfer catalysts. Shifting the pK(a) of the guanidinium analogues toward 7 was expected to raise catalytic activities in aqueous buffer. Although the pK(a)'s of both heterocycles are similar (6.2 and 7.0), only 2-aminobenzimidazole led to active RNA cleavers. All cleavage assays were run with fluorescently labeled substrates and a DNA sequencer. RNase contaminations would degrade RNA enantioselectively. In contrast, achiral catalysts such as 9b and 10b necessarily induce identical cleavage patterns in RNA and its mirror image. This principle allowed us to safely rule out contamination effects in this study. The most active catalysts, tris(2-aminobenzimidazoles) 9b and 1 Ob, were shown by fluorescence correlation spectroscopy (FCS) to aggregate with oligonucleotides. However, at very low concentrations the compounds are still active in the nonaggregated state. Conjugates of 10b with antisense oligonucleotides or RNA binding peptides, therefore, will be promising candidates as site specific artificial ribonucleases.