74447-69-1Relevant articles and documents
Pyrazole-Mediated C-H Functionalization of Arene and Heteroarenes for Aryl-(Hetero)aryl Cross-Coupling Reactions
Kundu, Abhishek,Dey, Dhananjay,Pal, Subhankar,Adhikari, Debashis
, p. 15665 - 15673 (2021/11/16)
Herein we introduce a transition-metal-free protocol that involves a commercially available, inexpensive pyrazole molecule to conduct C-C cross-coupling reactions at room temperature via a radical pathway. Using this method, an aryldiazonium salt has been coupled to a wide range of arenes and heteroarenes including benzene, mesitylene, thiophene, furan, benzoxazole to result the corresponding biaryl products. The full reaction mechanism is elucidated along with the crystallographic probation of an active initiator species. A potassium-stabilized deprotonated pyrazole steers single-electron transfer to the substrate and behaves as an initiator for the reaction.
Visible-Light-Promoted, Catalyst-Free Gomberg-Bachmann Reaction: Synthesis of Biaryls
Lee, Juyoung,Hong, Boseok,Lee, Anna
, p. 9297 - 9306 (2019/08/12)
Biaryls were synthesized via a novel visible-light-promoted Gomberg-Bachmann reaction that does not require a photosensitizer or any metal reagents. The formation of an electron donor-acceptor complex between aryl diazonium salts and pyridine allows, under visible-light irradiation, the synthesis of biaryls in moderate-to-high yields.
A process for preparing halogenated biphenyl (by machine translation)
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Paragraph 0029-0030, (2019/05/08)
A process for preparing halogenated biphenyl compound of the method, it is in order to aryl borate and aryl silane reagent as a raw material, 1, 1, 2 - trichloroethane as solvent, oxygenated esters of acetic acid as the oxidizing agent, paratoluene sulfonic acid silver as silver salts. In 110 °C lower, N - (diphenyl phosphate alkyl) - N - isopropyl - 1, 1 - diphenyl phosphine amine [...] 1 a catalytic cross-coupling, and efficient synthesis of aryl compounds of the halogenating is joint method. (by machine translation)
Palladium nanoparticles immobilized on the magnetic few layer graphene support as a highly efficient catalyst for ligand free Suzuki cross coupling and homo coupling reactions
Rafiee, Fatemeh,Khavari, Parvaneh,Payami, Zahra,Ansari, Narges
, p. 78 - 85 (2019/01/30)
In this study, we prepared a magnetic metal–graphene nanocomposite for the synthesis of substituted biaryls via Suzuki cross coupling and homo coupling reaction of aryl halides. The magnetic few layer graphene composite was synthesized by using one-step electrochemical exfoliation of graphite foil in aqueous iron (II) ammonium sulfate as electrolyte without using of any additive or corrosive media. Then, Fe2O3@FLG composite was used an efficient support for the immobilization and suitable dispersing of palladium nanoparticles. The obtained Fe2O3@FLG@Pd0 nanocomposite was characterized using FT-IR, SEM, TEM, EDS, XRD, VSM and ICP-AES analysis. Very low loading of this catalyst was displayed high activity in the producing substituted biaryls. It simply recovered from the reaction mixture and reused without any pre-activation in six consecutive runs with no loss of its catalytic activity or the observation of any detectable palladium leaching process.
ORGANIC LIGHT-EMITTING DIODE MATERIALS
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Paragraph 0559; 0560, (2018/08/09)
Described herin are molecules for use in organic light emitting diodes. Example molecules comprise at least one acceptor moiety A, at least one donor moiety D, and optionally one or more bridge moieties B. Each moiety A is covalently attached to either the moiety B or the moeity D, each moiety D is covalently attached to either the moeity B or the moeity A, and each B is covalently attached to at least one moiety A and at least one moiety D. Values and preferred values of moieties A, D and B are defined herein.
Structure-Affinity Relationships (SARs) and Structure-Kinetics Relationships (SKRs) of Kv11.1 Blockers
Yu, Zhiyi,Van Veldhoven, Jacobus P. D.,Louvel, Julien,'T Hart, Ingrid M. E.,Rook, Martin B.,Van Der Heyden, Marcel A. G.,Heitman, Laura H.,IJzerman, Adriaan P.
supporting information, p. 5916 - 5929 (2015/08/24)
Kv11.1 (hERG) blockers with comparable potencies but different binding kinetics might display divergent pro-arrhythmic risks. In the present study, we explored structure-kinetics relationships in four series of Kv11.1 blockers next to their structure-affinity relationships. We learned that despite dramatic differences in affinities and association rates, there were hardly any variations in the dissociation rate constants of these molecules with residence times (RTs) of a few minutes only. Hence, we synthesized 16 novel molecules, in particular in the pyridinium class of compounds, to further address this peculiar phenomenon. We found molecules with very short RTs (e.g., 0.34 min for 37) and much longer RTs (e.g., 105 min for 38). This enabled us to construct a kon-koff-KD kinetic map for all compounds and subsequently divide the map into four provisional quadrants, providing a possible framework for a further and more precise categorization of Kv11.1 blockers. Additionally, two representative compounds (21 and 38) were tested in patch clamp assays, and their RTs were linked to their functional IC50 values. Our findings strongly suggest the importance of the simultaneous study of ligand affinities and kinetic parameters, which may help to explain and predict Kv11.1-mediated cardiotoxicity.
17BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 INHIBITORS FOR THE TREATMENT OF HORMONE-RELATED DISEASES
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Page/Page column 32, (2011/04/14)
The invention relates to 17beta-hydroxysteroid dehydrogenase type 1 (17betaHSD1) inhibitors, the preparation thereof and the use thereof for the treatment and prophylaxis of hormone-related, especially estrogen-related or androgen-related, diseases.
Novel estrone mimetics with high 17β-HSD1 inhibitory activity
Oster, Alexander,Klein, Tobias,Werth, Ruth,Kruchten, Patricia,Bey, Emmanuel,Negri, Matthias,Marchais-Oberwinkler, Sandrine,Frotscher, Martin,Hartmann, Rolf W.
scheme or table, p. 3494 - 3505 (2010/10/19)
17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) catalyzes the reduction of estrone into estradiol, which is the most potent estrogen in humans. Lowering intracellular estradiol concentration by inhibition of this enzyme is a promising new option for th
Modulation of spectrokinetic properties of o-quinonoid reactive intermediates by electronic factors: Time-resolved laser flash and steady-state photolysis investigations of photochromic 6- and 7-arylchromenes
Moorthy, Jarugu Narasimha,Koner, Apurba L.,Samanta, Subhas,Roy, Ankur,Nau, Werner M.
supporting information; experimental part, p. 4289 - 4300 (2009/12/07)
A ready synthetic accessibility of a series of 6- and 7-arylchromenes via Pd0-catalyzed Suzuki coupling protocol has permitted a comprehensive investigation of the thermal decay behavior of a broad set of photogenerated o-quinonoid reactive intermediates. It is shown that substantial mesomeric effect between the benzopyran nucleus and the aryl ring at C6 or C7 position of the former renders significant absorption beyond 350 nm such that they are readily photoactivated to yield colored o-quinonoid intermediates. The absorption spectra of the latter are found to be strongly influenced by the substituents on C2-, C6- and C7-aryl rings; indeed the colored absorptions can be conveniently tuned by appropriate choice of substituents. The thermal decay (bleaching phenomenon), which is important from the point of view of their application in ophthalmic lenses, was investigated in each case by μs-ms as well as real-time absorption spec-troscopy. By careful experimentation, we have extracted the decay rate constants for Z,E and E,E o-quinonoid isomers of all 6- and 7-arylchromenes in an attempt to establish a correlation between the electronic attributes with their thermokinetic behavior. From a combined analysis of μs-ms (laser flash) and real-time kinetic data, it is shown that the colored o-quinonoid intermediates decay faster when the C2-aryl and C6-/C7-aryl rings contain electron-donating and electron-accepting groups, respectively. In the same vein, the decay was found to occur slowly for the reversed scenario, while intermediate decay rates are observed when both substituents are electron-donating. Thus, any substituent on the C2-aryl ring that contributes mesomerically to the development of charge on the quinonoid oxygen, and any substituent on the C6-/C7-aryl ring that exerts -I effect appear to expedite thermal decay. Furthermore, evidence is obtained for the first time from μs time-resolved laser-flash spectroscopy for the formation and characterization of the trans,cis (E,Z) o-quinonoid isomer, which has heretofore eluded spectral characterization in the photochromic phenomena of pyrans.
