33891-00-8Relevant academic research and scientific papers
Cleavage of 1,3-dicarbonyls through oxidative amidation
Biallas, Phillip,H?ring, Andreas P.,Kirsch, Stefan F.
supporting information, p. 3184 - 3187 (2017/04/21)
A mild and convenient protocol for the oxidative cleavage of 1,3-diketone compounds is described. Under metal-free conditions, the method converts the 1,3-dicarbonyls into amides when treated with (nBu4N)N3 and iodine in the presence of an amine at room temperature. Using this method, a range of 1,3-dicarbonyls with various structural motifs including sterically demanding substituents and ordinary functional groups were easily fragmented, and it is demonstrated that cyclic 1,3-dicarbonyls can be directly transformed into acyclic diamides through ring-opening. Initial mechanistic studies show that diazidation of the enol form is followed by nucleophilic substitution with the amine.
Combination of gold and iridium catalysts for the synthesis of N-alkylated amides from nitriles and alcohols
Li, Feng,Ma, Juan,Lu, Lei,Bao, Xiaofeng,Tang, Wanying
, p. 1953 - 1960 (2015/04/27)
An alternative and efficient approach for the synthesis of N-alkylated amides from nitriles and alcohols was proposed and accomplished. By the combination of [(IPr)Au(NTf2)] (IPr = 1,3-bis(diisopropylphenyl)imidazol-2-ylidene) and [CpIrCl2]2 (Cp = η5-pentamethylcyclopentadienyl), a series of nitriles were first hydrated to give amides, in which the resulting amides were further N-alkylated with a variety of alcohols as alkylating agents to afford N-alkylated amides with good to excellent yields. Compared with previous methods for the synthesis of N-alkylated amides from nitriles and alcohols as starting materials, this protocol could be accomplished with high atom economy under more environmentally benign conditions.
Design, synthesis, and biological evaluation of glycine-based molecular tongs as inhibitors of Aβ1-40 aggregation in vitro
Cellamare, Saverio,Stefanachi, Angela,Stolfa, Diana A.,Basile, Teodora,Catto, Marco,Campagna, Francesco,Sotelo, Eddy,Acquafredda, Pasquale,Carotti, Angelo
, p. 4810 - 4822 (2008/12/21)
A series of N-terminus benzamides of glycine-based symmetric peptides, linked to m-xylylenediamine and 3,4′-oxydianiline spacers, were prepared and tested as inhibitors of β-amyloid peptide Aβ1-40 aggregation in vitro. Compounds with good anti-
Synthesis of water-soluble diaza-1,2,5-thiadiazolo-cyclophanes
Hatta, Taizo,Kawano, Muneo,Imaizumi, Yuji,Tsuge, Akihiko,Moriguchi, Tetsuji,Maeda, Hironori,Tsuge, Otohiko
, p. 651 - 658 (2007/10/03)
The reaction of 3,4-bis(p-bromomethylphenyl)-1,2,5-thiadiazole (1) with bis(N-alkylaminomethyl)benzenes under high dilution conditions gave the diaza1,2,5-thiadiazolo[3.3.2]cyclophanes, while 1 reacted with xylylenediamines to give cupped diazathiadiazolo
