- THERAPEUTIC COMPOUNDS AND USES THEREOF
-
The present invention relates to compounds useful in the modulation of ion channel activity in cells. The invention also relates to use of these compounds in the treatment of pain, and pharmaceutical compositions containing these compounds and methods for their preparation.
- -
-
Page/Page column 52; 85
(2019/07/17)
-
- Catalyst-Free Transamidation of Aromatic Amines with Formamide Derivatives and Tertiary Amides with Aliphatic Amines
-
A simple catalyst- and promoter-free protocol has been developed for the transamidation of weakly nucleophilic aromatic amines with formamide derivatives and low-reactivity tertiary amides with aliphatic amines. This strategy is advantageous because no catalyst or promoters are needed, no additives are required, separation and purification is easy, and the reaction is scalable. Significantly, this strategy was further applied to synthesize several pharmaceutical molecules on a gram scale, and excellent yields were achieved.
- Yin, Jiawen,Zhang, Jingyu,Cai, Changqun,Deng, Guo-Jun,Gong, Hang
-
supporting information
p. 387 - 392
(2019/01/11)
-
- A non-catalyst non-promoter under the conditions of amide derivatives of aromatic amine with transfers the amine reaction
-
The present invention discloses a non-catalyst under the condition of non-accelerator [...] amide derivatives of aromatic amine with transfers the amine reaction, yield of synthetic N - aryl amide derivatives. The method has a wide range of the substrate, its raw materials and cheap and easy to obtain acylation reagent, the reaction yield is high, one-step reaction, low cost, high reaction selectivity, simple operation and the like. Adopting this method can be gram scale can realize the high yield of the synthesis of drug molecules. Therefore, the method in the N - aryl amide derivatives of synthesis application field has very good application prospect. The method overcomes the existing technologies such as the reaction reagent toxicity is large, the need to use different type catalyst, synthesis method and the cost is high, more reaction steps, more byproducts and the like.
- -
-
Paragraph 0039; 0040
(2019/03/28)
-
- Air-stable Bis(pentamethylcyclopentadienyl) Zirconium Perfluorooctanesulfonate as an Efficient and Recyclable Catalyst for the Synthesis of N-substituted Amides
-
Bis(pentamethylcyclopentadienyl) zirconium perfluorooctanesulfonate is an air-stable and water-tolerant Lewis acid. This complex exhibited good thermal stability and high solubility in polar organic solvents. The compound showed relatively strong acidity, with an acid strength of 0.8Ho≤3.3, and high catalytic efficiency for the synthesis of N-substituted amides via the reaction of carboxylic acids with amines, the Ritter reaction of nitriles with alcohols, and the amination of alcohols with amides. Moreover, the complex had good reusability. This catalytic system affords a simple and efficient way to synthesize N-substituted amides.
- Li, Ningbo,Wang, Lingxiao,Zhang, Liting,Zhao, Wenjie,Qiao, Jie,Xu, Xinhua,Liang, Zhiwu
-
p. 3532 - 3538
(2018/08/01)
-
- Cu-Catalyzed Intramolecular Amidation of Unactivated C(sp3)-H Bonds to Synthesize N-Substituted Indolines
-
A copper-catalyzed intramolecular amidation of unactivated C(sp3)-H bonds to construct indoline derivatives has been developed. Such an amidation proceeded well at primary C-H bonds preferred to secondary C-H bonds. The transformation owned a b
- Pan, Fei,Wu, Bin,Shi, Zhang-Jie
-
supporting information
p. 6487 - 6490
(2016/05/02)
-
- Palladium-catalyzed C(sp2)-H arylation using formamide as a transformable directing group
-
A new process for the ortho arylation of formanilides through palladium-catalyzed C-H activation is described. Formamide is reported as a transformable directing group in the transition-metal-catalyzed C-H functionalization reaction. The resulting biarylformanilide products can be readily transformed to the corresponding biarylisocyanides or N-heterocycles.
- Wan, Congqing,Zhao, Jiaji,Xu, Mingfang,Huang, Jinbo
-
p. 4751 - 4756
(2014/06/09)
-
- Palladium-catalyzed intramolecular C(sp2)-H amidination by isonitrile insertion provides direct access to 4-aminoquinazolines from N-arylamidines
-
An efficient method for the synthesis of 4-amino-2-aryl(alkyl)quinazolines from readily available N-arylamidines and isonitriles via palladium-catalyzed intramolecular aryl C-H amidination by isonitrile insertion has been developed.
- Wang, Yong,Wang, Honggen,Peng, Jiangling,Zhu, Qiang
-
supporting information; experimental part
p. 4604 - 4607
(2011/10/12)
-
- Screw Sense Selective Polymerization of Achiral Isocyanides Catalysed by Optically Active Nickel(II) Complexes
-
Poly(isocyanides), (RN=Cn, can be prepared from isocyanides, , by the catalytic action of nickel(II) compounds.The main chain of these polymers is a rigid helix.This helical conformation results from a restricted rotation around the single bonds that connect the main-chain carbon atoms.Polymerization of achiral isocyanides generally gives a racemic mixture of left- and right-handed helices, whereas polymerization of optically active isocyanides results in helices with an excess of one screw sense.We describe a procedure for obtaining poly(isocyanides) with predominantly one screw sense, starting from an achiral monomer.A catalyst is prepared by adding an optically active amine to a tetrakis(isocyanide)nickel(II) perchlorate complex.Polymerization of various achiral isocyanides with this catalist yields optically active polymers with an enantiomeric excess up to 83percent.
- Kamer, Paul C. J.,Nolte, Roeland J. M.,Drenth, Wiendelt
-
p. 6818 - 6825
(2007/10/02)
-
- The Isonitrile-Nitrile Rearrangement. A Reaction without a Structure-Reactivity Relationship
-
Reproducible rates of isomerisation of aliphatic isonitriles to nitriles in solution can be measured by GLC or IR when free-radical inhibitors are added to suppress a competing radical chain reaction.The reactivities of 19 primary, secondary, tertiary, cyclic, bicyclic, bridgehead, benzyl, substituted-benzyl, α-carbomethoxymethyl, and triphenylmethyl isocyanides in this rearrangement reaction vary by only a factor of 67 in rate or by +/- 2 kcal mol-1 in ΔG(excit.).This is explained by a tight hypervalent three-membered cyclic transition state in agreement with a previous prediction by ab initio calculation.The slower rate of 9-triptycyl isocyanide is proposed to be due to steric hindrance by the three peri hydrogens.Aromatic isocyanides isomerize about 10 times faster independent of polar para substituents and bulky ortho substituents.A hypervalent orthogonal transition state with retention of the aromatic sextet is proposed in contrast to the popular phenonium-type transition states for aryl migration in other 1,2-rearrangements.The reactivity data and the transition-state structures are discussed in context with other cationotropic 1,2-shifts.
- Meier, Michael,Mueller, Barbara,Ruechardt, Christoph
-
p. 648 - 652
(2007/10/02)
-