592552-31-3Relevant academic research and scientific papers
Tandem Long Distance Chain-Walking/Cyclization via RuH2(CO)(PPh3)3/Br?nsted Acid Catalysis: Entry to Aromatic Oxazaheterocycles
Bernárdez, Rodrigo,Suárez, Jaime,Fa?anás-Mastral, Martín,Varela, Jesús A.,Saá, Carlos
, p. 642 - 645 (2016)
A novel route to 1,3-oxazaheterocycles based on cooperative Ru-H/Br?nsted acid catalysis is reported. The use of the commercially available RuH2(CO)(PPh3)3 complex allows for an efficient long distance chain-walking process while the Br?nsted acid is responsible for generation of an electrophilic iminium ion which is trapped intramolecularly by an alcohol moiety. The alcohol, besides its nucleophilic function, also plays an important role in the stabilization of the Ru catalyst. (Chemical Equation Presented).
Synthesis of the analogs of plocabulin and their preliminary structure-activity relationship study
Wang, Leiming,Li, Xin,Cui, Hong,Lei, Xinsheng,Liu, Hongchun,Wang, Quanrui,Li, Yingxia
supporting information, (2021/09/28)
Plocabulin, a marine natural polyketide isolated from the sponge Lithoplocamia lithistoides, is a novel and potent microtubule-destabilizing agent. Guided by the reported binding mode, several new analogs of plocabulin have been designed through removing
Small Molecule Inhibitors of KRAS G12C Mutant
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Paragraph 0330-0331, (2021/04/30)
The disclosure provides compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein W1, W2, Y, Z, M, L, Cy, Cz, R1, R2, R3, R4, R2a, Rs
INHIBITORS OF CYTOKININ OXIDASE DERIVED FROM 1-[2-(HYDROXYALKYL)PHENYL]-3-YLUREA, USE THEREOF AND PREPARATIONS CONTAINING THESE DERIVATIVES
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Page/Page column 29, (2021/09/26)
The present invention relates to substituted 1-[2-(hydroxyalkyl)phenyl]-3-yl-urea derivatives of the general formula (I), which inhibit one of the key plant enzymes cytokinin oxidase/dehydrogenase (CKX); wherein R1 is hydrogen, halogen, methoxy group, trifluoromethoxy group, methylsulphanyl group or trifluoromethylsulphanyl group; R2 is hydrogen, halogen, amino group, (C1-C5) alkyl, (C2-C5) alkenyl, (C2-C5) alkynyl, or (C1-C5) alkylamino group, wherein (C1-C5) alkyl, (C2-C5) alkenyl, (C2-C5) alkynyl and (C-C5) alkylamino group is optionally substituted with hydroxy and/or amino group; and R3 and R4 are independently hydrogen or halogen, and wherein when X is nitrogen, then R2 is hydrogen or halogen. The invention further relates to the use of these substances in agriculture as stimulators of plant growth and development and as anti-stress factors and to the preparations containing these derivatives.
Iridium-catalyzed regioselective silylation of aromatic and benzylic C-H bonds directed by a secondary amine
Li, Qian,Driess, Matthias,Hartwig, John F.
supporting information, p. 8471 - 8474 (2014/08/18)
Reported herein is an iridium-catalyzed, regioselective silylation of the aromatic C-H bonds of benzylamines and the benzylic C-H bonds of 2,N-dialkylanilines. In this process, (hydrido)silyl amines, generated in situ by dehydrogenative coupling of benzylamine or aniline with diethylsilane, undergo selective silylation at the C-H bond γ to the amino group. The products of this silylation are suitable for subsequent oxidation, halogenation, and cross-coupling reactions to deliver benzylamine and arylamine derivatives.
Pyrrolidinyl phenylurea derivatives as novel CCR3 antagonists
Nitta, Aiko,Iura, Yosuke,Inoue, Hideki,Imaoka, Takayuki,Takahashi, Toshiya,Sato, Ippei,Morihira, Koichiro,Kubota, Hirokazu,Morokata, Tatsuaki,Takeuchi, Makoto,Ohta, Mitsuaki,Tsukamoto, Shin-Ichi
, p. 6876 - 6881,6 (2020/09/02)
Optimization starting with our lead compound 1 (IC50 = 4.9 nM) led to the identification of pyrrolidinyl phenylurea derivatives. Further modification toward improvement of the bioavailability provided (R)-1-(1-((6-fluoronaphthalen-2-yl)methyl)pyrrolidin-3-yl)-3-(2-(2- hydroxyethoxy)phenyl)urea 32 (IC50 = 1.7 nM), a potent and orally active CCR3 antagonist.
Photochemical generation of iminoquinone methides by 1,4-hydrogen migration in derivatives of o-tolylnitrene
Bucher, Goetz
, p. 2447 - 2462 (2007/10/03)
The photochemistry of a series of derivatives of o-tolyl azide, bearing a variety of substituents in the benzylic positions, has been investigated using matrix isolation spectroscopy and density functional calculations. It has been found that introduction of any substituent possessing a lone pair (i.e., R = Br, Cl, MeO, Me2N) allows a 1,4-hydrogen shift to take place, yielding iminoquinone methides. Additional methyl groups in the benzylic position, however, do not promote a photochemical conversion into iminoquinone methides. If the benzylic substituent itself is part of a ring system, the size of this ring plays an important role. Thus, 2-methyl-8-nitrenote-trahydroisoquinoline rearranges very easily, whereas 4-nitrenophthalan does not give the reaction. Density functional calculations [B3LYP/6-31G(d)] have been used to gain an understanding of the reaction. It has been found that the activation energies depend strongly on the nature of the substituent, being lowest if R = NMe2. Incorporation of the benzylic substituent into a ring reduces the flexibility of the system and results in significantly raised barriers.
