36804-50-9Relevant academic research and scientific papers
Palladium-catalyzed synthesis of α-aryl acetophenones from styryl ethers and aryl diazonium saltsviaregioselective Heck arylation at room temperature
Venkatesh, Rapelly,Singh, Adesh Kumar,Lee, Yong Rok,Kandasamy, Jeyakumar
, p. 7832 - 7837 (2021/09/28)
Preparation of α-aryl acetophenones from styryl ethers and aryldiazonium salts is described. The reaction is catalyzed by palladium acetate at room temperature in the absence of ligand and base. The developed method is highly attractive in terms of reaction conditions, substrate scope, functional group tolerance and yields. Synthetic applications of the present method are demonstrated by preparing α-aryl indoles and 3-aryl isocoumarin from styryl ethers.
Sequential Sonogashira/intramolecular aminopalladation/cross-coupling ofortho-ethynyl-anilines catalyzed by a single palladium source: rapid access to 2,3-diarylindoles
Wang, Jiwei,Wang, Gendi,Cheng, Xiang,Liu, Ye,Zhang, Jun
, p. 1329 - 1333 (2021/02/26)
We have developed a practical and efficient one-pot protocol for the synthesis of 2,3-diarylindolesviaPd-catalyzed bis-arylative cyclization of variouso-ethynylanilines with aryl iodides. Mechanism studies showed that a Pd-catalyzed Sonogashira reaction took place firstly, giving an internal alkyne intermediate, which subsequently underwent intramolecular aminopalladation/cross-coupling to give access to 2,3-diarylindoles. The present methodology exhibits a broad substrate scope, producing various 2,3-diaryl indoles bearing two different aryl groups.
Synthesis of Unprotected and Highly Substituted Indoles by the Ruthenium(II)-Catalyzed Reaction of Phenyl Isocyanates with Diaryl/Diheteroaryl Alkynes/Ethyl-3-phenyl Propiolates
Kumar, Amrendra,Tadigoppula, Narender
supporting information, p. 8 - 12 (2021/01/13)
A one-pot transformation has been developed for the synthesis of unprotected and highly substituted indoles by an in situ installed carbamide-directed Ru(II)-catalyzed intermolecular oxidative annulation of phenyl isocyanates with diaryl/diheteroaryl alkynes/ethyl phenyl propiolates in the presence of Cu(OAc)2·H2O as an oxidant and AgSbF6 as an additive at 120 °C within 3 h.
Step and redox efficient nitroarene to indole synthesis
?zkaya, Bünyamin,Bub, Christina L.,Patureau, Frederic W.
supporting information, p. 13185 - 13188 (2020/11/09)
Step and redox efficiencies are a rising priority in synthetic method development, in order to make synthetic processes more sustainable and more affordable. Herein, a step and redox efficient nitroarene to indole synthesis is developed, in sharp contrast to the rich literature on the construction of indoles. Elemental zinc was found to be the best terminal reductant. This journal is
Method for preparing indole compounds by using rhodium/carbon as catalyst
-
Paragraph 0029-0031; 0034; 0036, (2018/04/26)
The invention provides a method for preparing indole compounds by using rhodium/carbon as a catalyst. Corresponding indole compounds are formed through subjecting aniline and analogs thereof and alkyne to a catalytic cyclization reaction in the presence of the rhodium/carbon. The method has the beneficial effects that the preparation method is simple in process, the raw materials are cheap and readily available, the yield is high, inert-gas protection is not required, and the reaction temperature is relatively moderate.
A palladium/carbon as catalyst preparation of indole compounds method (by machine translation)
-
Paragraph 0029; 0030; 0031; 0033, (2018/06/15)
The present invention provides a palladium/carbon as catalyst preparation of indole compounds method, aniline and its analogs in the palladium/carbon with the alkyne under the action of the catalytic cyclization reaction, to form the corresponding indoles. This method has the advantages of: simple preparation method, the raw material is cheap, high yield, without protection of inert gas, the reaction temperature is relatively mild. (by machine translation)
N, N-Dimethylformamide-stabilized palladium nanoclusters as a catalyst for Larock indole synthesis
Onishi, Kaito,Oikawa, Kei,Yano, Hiroki,Suzuki, Takeyuki,Obora, Yasushi
, p. 11324 - 11329 (2018/04/05)
We show that N,N-dimethylformamide-stabilized Pd nanoclusters (NCs) have high catalytic activity in the reaction of substituted 2-iodoanilines with alkynes to give 2,3-disubstituted indoles. This indole synthesis does not require phosphine ligands and proceeds with low Pd catalyst loadings. The Pd NCs were separated from the mixture after the reaction, and recycled at least three times. Transmission electron microscopy images showed that the Pd particle size before the reaction was 1.5-2.5 nm. The particle size after the reaction was 2-3 nm. X-ray photoelectron spectroscopy showed that the binding energy of the Pd NCs before the reaction was 335.0 eV.
Selective Synthesis of Indoles by Cobalt(III)-Catalyzed C-H/N-O Functionalization with Nitrones
Wang, Hui,Moselage, Marc,González, María J.,Ackermann, Lutz
, p. 2705 - 2709 (2016/04/26)
The redox-neutral annulation of alkynes by differently decorated nitrones set the stage for a step-economical access to indoles with ample substrate scope. The redox-neutral C-H/N-O functionalization process proceeded through kinetically relevant C-H activation by carboxylate assistance, and displayed an excellent site- and regio-selectivity with unsymmetrical nitrones and alkynes.
A kind of high-efficient synthetic indole and isoquinoline derivatives (by machine translation)
-
Paragraph 0029; 0030, (2016/10/07)
The invention discloses a substituted indole and isoquinoline preparation method, which belongs to the technical field of organic chemical synthesis. This method adopts the oxygen as the oxidizing agent, various substituents substituted alkyne starting material of the aromatic amine or [...] , by transition metal-catalyzed, get containing indole or isoquinoline compound of the structure. The reaction raw material, oxidizing agent and cheap and easily obtained catalyst, synthesis technique is simple, which greatly reduces the cost of synthesizing; mild reaction conditions, high yield, easy industrialization; reaction raw materials and catalyst cleaning non-toxic, small pollution to the environment. Such compounds and their derivatives as an important fine chemicals, in the medical, agricultural chemicals, perfume and widely used photoelectric and other industries. (by machine translation)
INDOLE DERIVATIVE OR SALT THEREOF
-
Paragraph 0050, (2020/04/17)
PROBLEM TO BE SOLVED: To provide a compound that has excellent aP2 inhibitory action and is useful as medicaments, aP2 inhibitors, and therapeutics for the diseases improved by the inhibition of aP2. SOLUTION: The problem is solved by a compound represented by the general formula (I) (for symbols in the formula, refer to definitions in the specifications) or salt thereof. COPYRIGHT: (C)2015,JPOandINPIT
