- Acceleration of the Passerini reaction in the presence of nucleophilic additives
-
An accelerating effect of nucleophilic additives was revealed for the Passerini multi-component reaction. The influence of aqueous solutions on the reaction rate was studied in detail and the direct involvement of water in the bond-making step was attributed as the basis of an accelerating effect. Other nucleophiles were tested as alternatives to water; as a result N-hydroxysuccinimide is proposed as an accelerant of the Passerini reaction.
- Mironov, Maxim A.,Ivantsova, Maria N.,Tokareva, Maria I.,Mokrushin, Vladimir S.
-
-
Read Online
- CANCER TREATMENTS TARGETING CANCER STEM CELLS
-
Disclosed are compounds, methods, compositions, and kits that allow for treating cancer by, e.g., targeting cancer stem cells. In some embodiments, the cancer is colorectal cancer, gastric cancer, gastrointestinal stromal tumor, ovarian cancer, lung cancer, breast cancer, pancreatic cancer, prostate cancer, testicular cancer, or lymphoma. In some embodiments, the cancer is liver cancer, endometrial cancer, leukemia, or multiple myeloma. The compounds utilized in the disclosure are of Formula (0), (O'), and (I):
- -
-
Paragraph 0331; 0421-0423
(2019/11/19)
-
- Formamide Synthesis through Borinic Acid Catalysed Transamidation under Mild Conditions
-
A highly efficient and mild transamidation of amides with amines co-catalysed by borinic acid and acetic acid has been reported. A wide range of functionalised formamides was synthesized in excellent yields, including important chiral α-amino acid derivatives, with minor racemisation being observed. Experiments suggested that the reaction rely on a cooperative catalysis involving an enhanced boron-derived Lewis acidity rather than an improved Br?nsted acidity of acetic acid. Amide bonds are reputedly difficult to activate due to their high resonance stabilization. An unusual mild activation of dimethylformamide and formamide by borinic acid 1 (see scheme), illustrated by a general formylation of a wide range of amines, including chiral α-amino esters, has been reported.
- Mohy El Dine, Tharwat,Evans, David,Rouden, Jacques,Blanchet, Jér?me
-
supporting information
p. 5894 - 5898
(2016/04/26)
-
- Synthesis of pyrrolidones and quinolines from the known biomass feedstock levulinic acid and amines
-
The catalytic conversion of biomass-derived compounds into value-added products such as food additives, agrochemical components, and pharmaceutical formulations, is a promising and cost effective synthetic strategy. Here, we describe the synthesis of a variety of N-(alkyl, aryl)-5-methyl-2-pyrrolidones through the reductive amination of levulinic acid using formic acid as the hydrogen source. This system is catalyzed by 3.8 nm ruthenium nanoparticles that were prepared by thermal decomposition of [Ru3(CO)12] in solvent-free conditions. When the reactions were carried out without the catalyst, the pyrrolidones were obtained with low yield and poor selectivity. In addition, the reaction between levulinic acid and 2-ethynylaniline produced 2-(2,4-dimethylquinolin-3-yl) acetic acid (8) in mild and metal-free conditions with good yield. Furthermore, the synthesis of substituted quinolines was achieved through a condensation reaction between levulinic acid and different 2-alkynylanilines promoted by p-toluenesulfonic acid, this method is highlighted as a novel procedure for the preparation of quinolines.
- Ortiz-Cervantes, Carmen,Flores-Alamo, Marcos,García, Juventino J.
-
supporting information
p. 766 - 771
(2016/02/05)
-
- Hydrogen acceptor- and base-free N-formylation of nitriles and amines using methanol as C1 source
-
An N-formylation method using methanol as the C1 source without a stoichiometric amount of activating reagent is described. Nitriles as well as amines can be directly used as substrates. The reaction is catalyzed by an N-heterocyclic carbene coordinated ruthenium(II) dihydride complex, which mediates methanol dehydrogenation, nitrile reduction, and C-N bond formation without any external base, hydrogen acceptor, or oxidant.
- Kang, Byungjoon,Hong, Soon Hyeok
-
supporting information
p. 834 - 840
(2015/03/18)
-
- Benzoic acid-catalyzed transamidation reactions of carboxamides, phthalimide, ureas and thioamide with amines
-
An efficient and simple method for the transamidation of carboxamides, phthalimide, ureas and thioamide with amines catalyzed by commercially available benzoic acid under metal-free conditions is described. Furthermore, to the best of our knowledge, this is the first report about the transamidation of an aromatic thioamide with amines.
- Wu, Ji-Wei,Wu, Ya-Dong,Dai, Jian-Jun,Xu, Hua-Jian
-
supporting information
p. 2429 - 2436
(2014/09/30)
-
- Formylation of amines through catalyst- and solvent-free transamidation reaction
-
The transamidation between formamide and various amines proceeds under heating, without any catalyst nor solvent, providing thus green and neutral conditions for the formylation of primary and secondary amines. The resulting amide product can be directly transformed, in a one pot sequence, into monomethylamine.
- Lebleu, Thomas,Kotsuki, Hiyoshizo,Maddaluno, Jacques,Legros, Julien
-
supporting information
p. 362 - 364
(2014/01/06)
-