Large-Scale Synthesis of Symmetric Tetramine Ligands by Using a Modular Double Reductive Amination Approach
作者:Maik Tretbar、Christian B. W. Stark
DOI:10.1002/ejoc.201700772
日期:2017.12.15
Tetramine ligands play an important role in a broad range of transition metal catalyzed transformations. We here present a flexible and modular approach to this class of ligands using a double reductive aminationstrategy. Thus, the target molecules were prepared in a highly efficient manner in only three steps, from commercially available starting materials. Excellent overall yields, of up to 96 %
四胺配体在广泛的过渡金属催化转化中发挥重要作用。我们在这里使用双还原胺化策略对此类配体提出了一种灵活且模块化的方法。因此,目标分子仅通过三个步骤以高效方式从市售原料制备。达到了高达 96% 的优异总产率。值得注意的是,使用此程序可以获得手性 C 2 对称配体。所有反应都可以轻松扩展,并且以优异的纯度获得了四胺配体,而在三步序列结束时只需要一次色谱纯化。
PLATINUM COMPOUND HAVING AMINO OR ALKYLAMINO-CONTAINING SUCCINIC ACID DERIVATIVES AS LEAVING GROUP, PREPARTION METHOD THEREOF, AND USE THEREOF
申请人:BEIJING FSWELCOME TECHNOLOGY DEVELOPMENT CO., LTD.
公开号:US20140349985A1
公开(公告)日:2014-11-27
Disclosed are a category of platinum compounds having amino- or alkylamino-containing succinato derivatives as leaving group, or pharmaceutically acceptable salts thereof, preparation method thereof, and medicinal compositions containing the compounds. Also disclosed is a use of the compounds in treating cell proliferative diseases, especially cancers. The platinum compounds of the present invention have high water solubility and small toxic side effect.
Synthesis and analysis of the anticancer activity of platinum(<scp>ii</scp>) complexes incorporating dipyridoquinoxaline variants
作者:Benjamin J. Pages、Feng Li、Paul Wormell、Dale L. Ang、Jack K. Clegg、Cameron J. Kepert、Lawson K. Spare、Supawich Danchaiwijit、Janice R. Aldrich-Wright
DOI:10.1039/c4dt02133a
日期:——
Platinum complexes incorporating variants of dpq were synthesised. Their DNA affinity and cytotoxicity were compared to complexes containing phen variants, revealing unexpected trends in biological activity.
A straightforward chemoenzymaticsynthesis of optically active trans-N,N-dialkylcyclopentane-1,2-diamines has been efficiently developed starting out from their analogous (±)-trans-2-(N,N-dialkylamino)cyclopentanols. The route involves the one-pot stereospecific transformation of the racemic amino alcohols into racemic diamines and a subsequent kinetic resolution by means of lipase-B from Candida
作者:Douglas Lloyd、Ronald H. McDougall、Donald R. Marshall
DOI:10.1039/j39660000780
日期:——
open-chain condensation products result. Glycinamide reacts with acetyl-acetone to give an azomethine rather than a diazepine. Perhydro-1,4-diazepine could not be dehydrogenated to a dihydrodiazepine. The 2,3-dihydro-1H-1,4-diazepinium cation is very stable, as evinced by the pK values of the diazepine and by its relative stability to permanganate oxidation.
当将β-二酮和脂肪族1,2-二胺的等摩尔混合物在乙酸中加热时,会形成2,3-二氢-1 H -1,4-二氮杂derivatives衍生物。但是,如果将这些反应物的2:1混合物保持在室温下(无论是在醇中还是在无溶剂中),都将产生开链缩合产物。甘氨酰胺与乙酰丙酮反应生成偶氮甲碱而不是二氮杂pine。过氢的1,4-二氮杂pine不能脱氢成二氢二氮杂pine。2,3-二氢-1 H -1,4-二氮杂吡啶鎓阳离子非常稳定,这是由二氮杂的p K值及其对高锰酸盐氧化的相对稳定性所证明的。