2437-43-6Relevant academic research and scientific papers
A solvent-free manganese(II) -catalyzed Clauson-Kaas protocol for the synthesis of N-aryl pyrroles under microwave irradiation
Rohit, Kizhakkekuttu Radhakrishnan,Meera, Gopinadh,Anilkumar, Gopinathan
supporting information, p. 194 - 200 (2021/10/12)
The first manganese-catalyzed modified Clauson-Kaas reaction for N-substituted pyrrole synthesis using 2,5-dimethoxytetrahydrofuran with variously substituted aromatic amines has been developed (up to 89% yield). This interesting neat strategy is free from additives including co-catalysts, ligands, and acids. Relatively low cost, environmentally benign, and handy Mn(NO3)2·4H2O is employed as the catalyst under microwave conditions with a very short reaction time (20?min). The above qualities attest to the green nature of this reaction.
Utilization of caffeine carbon supported cobalt catalyst in the tandem synthesis of pyrroles from nitroarenes and alkenyl diols
Balasubramaniam, Bhuvaneshwari,Dhara, Partha,Gupta, Raju K.,Kundu, Sabuj,Panja, Dibyajyoti,Sau, Anirban
, p. 244 - 254 (2021/09/07)
Employing bio-waste caffeine carbon-supported heterogeneous cobalt catalyst, synthesis of various substituted pyrrole derivatives is reported. In this methodology, pyrroles were synthesized through coupling between nitroarenes and alkenyl diols in a tandem manner. Among all the heterogeneous catalysts Co(OAc)2-CC-800 displayed the highest catalytic activity. Preparative scale synthesis of pyrroles and synthesis of anti-tubercular agent 5-(4-(1H-pyrrol-1-yl)phenyl)-1,3,4-oxadiazole-2-thiol revealed the practical applicability of this protocol. Several kinetic experiments and Hammett studies were conducted to understand the probable mechanism and electronic effects on this transformation.
Lactam derivatives and preparation method and application thereof
-
Paragraph 0048-0052; 0076; 0083, (2020/02/10)
The invention relates to lactam derivatives and a preparation method and application thereof. Compared with the prior art, the invention provides lactam compounds with a novel structure. The compoundsand compositions thereof have remarkable activity in inhibition of the proliferation of cancer cells (including, but not limited to, the liver cancer cell line HepG2 and the lung cancer cell line A549), and the activity of multiple compounds is in the same order of magnitude as the activity of the commercial drug adriamycin or superior to the activity of adriamycin. The compounds of the inventioncan be prepared from N-substituted pyrrole compounds through a reaction, and the preparation method is convenient, rapid and efficient.
Pd/Cu-catalyzed dual C-H bond carbonylation towards the synthesis of fluorazones
Liao, Fan,Shi, Renyi,Sha, Yuchen,Xia, Jianhui,Liao, Weilin,Lei, Aiwen
supporting information, p. 4354 - 4357 (2017/04/21)
Pd/Cu catalyzed oxidative dual C-H bond activation/carbonylation still remains a great challenge due to the generation of by-products via C-C bond formation. Herein we developed a straightforward Pd/Cu-catalyzed oxidative dual C-H bond carbonylation process to access biologically and pharmaceutically important fluorazones from easily available N-aryl pyrroles and CO. A wide range of functional groups were well tolerated in this transformation, and O2 could be utilized as the only terminal oxidant to promote the oxidative carbonylation process.
Natural polynite promote nitrogen heterocyclic compound N-arylation of the method
-
Paragraph 0011, (2016/10/31)
The invention discloses a method of promoting N-arylation of nitrogen heterocyclic compounds by natural montmorillonite. The natural montmorillonite is adopted as a promoter and cuprous iodide or copper acetate is adopted as a catalyst, and under alkaline
An efficient heterogeneous catalytic method for the N-arylation of pyrrole and other N-heterocycles
Nmeth, Jnos,Debreczeni, Nra,Gresits, Ivn,Blint, Mria,Hell, Zoltn
, p. 1113 - 1119 (2015/08/06)
Abstract 4 ? molecular sieve modified with copper(0) or copper(II) is an efficient heterogeneous catalyst for the arylation of pyrrole and some other heterocycles with iodo- or bromoarenes, Cs2CO3 base and pyrrole (or DMF) solvent. The catalysts can be easily prepared and are reusable.
Buchwald-Hartwig reactions in water using surfactants
Salomé, Christophe,Wagner, Patrick,Bollenbach, Maud,Bihel, Frédéric,Bourguignon, Jean-Jacques,Schmitt, Martine
, p. 3413 - 3421 (2014/05/06)
Examination of the scope and limitation of the Buchwald-Hartwig cross-coupling reaction in micellar medium is reported. An array of aryl or heteroaryl halides were coupled to diverse nitrogen coupling partners using a combination of [(allyl)PdCl]2 and cBRIDP to afford the corresponding products in moderate to excellent yields. 30 examples are reported, including polar solid and fairly water-soluble organic substrates/reagents.
Nano sulfated titania as a heterogeneous solid acid catalyst for the synthesis of pyrroles by clauson-kaas condensation under solvent-free conditions
Hosseini-Sarvari,Najafvand-Derikvandi,Jarrahpour,Heiran
, p. 1732 - 1739 (2014/05/06)
A new and environmentally benign method for the preparation of N-substituted pyrroles from one-pot condensation reaction of 2,5-dimethoxytetrahydrofuran with amines and diamines in the presence of nano sulfated titania under solvent-free conditions is presented. This new protocol features simple operation, easy availability, stability, and eco-friendliness of catalyst, as well as high to excellent yields of products. In addition, we report for the first time an alternative method for the synthesis of pyrroles from aromatic amines containing the β-lactam fragment using nano sulfated titania as catalyst.
New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer
La Regina, Giuseppe,Bai, Ruoli,Coluccia, Antonio,Famiglini, Valeria,Pelliccia, Sveva,Passacantilli, Sara,Mazzoccoli, Carmela,Ruggieri, Vitalba,Sisinni, Lorenza,Bolognesi, Alessio,Rensen, Whilelmina Maria,Miele, Andrea,Nalli, Marianna,Alfonsi, Romina,Di Marcotullio, Lucia,Gulino, Alberto,Brancale, Andrea,Novellino, Ettore,Dondio, Giulio,Vultaggio, Stefania,Varasi, Mario,Mercurio, Ciro,Hamel, Ernest,Lavia, Patrizia,Silvestri, Romano
, p. 6531 - 6552 (2014/10/16)
We synthesized 3-aroyl-1-arylpyrrole (ARAP) derivatives as potential anticancer agents having different substituents at the pendant 1-phenyl ring. Both the 1-phenyl ring and 3-(3,4,5-trimethoxyphenyl)carbonyl moieties were mandatory to achieve potent inhi
Synthesis of pyrrole derivatives from diallylamines by one-pot tandem ring-closing metathesis and metal-catalyzed oxidative dehydrogenation
Chen, Weiqiang,Wang, Jianhui
supporting information, p. 1958 - 1963 (2013/05/08)
A series of aryl-substituted pyrrole derivatives was synthesized from diallylamines through a ruthenium carbene catalyzed ring-closing metathesis reaction and in situ oxidative dehydrogenation reaction catalyzed by FeCl 3·6H2O or CuCl2·2H2O in the presence of O2. The reaction was mild, simple, and convenient. An oxygen atmosphere played a critical role in obtaining high conversion of substituted pyrroles in the proposed catalytic system.
