10292-65-6Relevant academic research and scientific papers
Bcl-2 INHIBITORS
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Paragraph 0804; 0805, (2019/11/19)
Disclosed herein is a compound of Formula (I) for inhibiting Bcl-2 and treating disease associated with undesirable bcl-2 activity (Bcl-2 related diseases), a method of using the compounds disclosed herein for treating dysregulated apoptotic diseases including cancers and treating autoimmune disease, and a pharmaceutical composition comprising the same.
SUBSTITUTED TRICYCLIC COMPOUNDS WITH ACTIVITY TOWARDS EP1 RECEPTORS
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Page/Page column 41, (2013/10/22)
The present invention belongs to the field of EP1 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP1 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP1 receptor as well as to pharmaceutical compositions comprising them.
Facile synthesis of aryl(het)cyclopropane catalyzed by palladacycle
Zhang, Min,Cui, Xiuling,Chen, Xiaopei,Wang, Lianhui,Li, Jingya,Wu, Yusheng,Hou, Lifen,Wu, Yangjie
experimental part, p. 900 - 905 (2012/02/01)
Sphos (2-dicyclohexylphosphino-2′,6′-dimethoxy-1,1′- biphenyl) adduct of cyclopalladated ferrocenylimine (IIe) exhibited highly catalytic activity for the Suzuki cross-coupling reaction of cyclopropylboronic acid with aryl(het) halides with 1 mol % catalyst loading. This process was applied to both of aryl and heteroaryl halides (Br and Cl), and made the various arylcyclopropane and heteroarylcyclopropane to be easily synthesized. A variety of substituents on the aryl halides, such as alkyl, acetyl, benzoyl, ether, formyl, carboxylate, methoxy, nitro and cyano were tolerated.
Radical ion probes. Part 10. Ceric(IV) ammonium nitrate oxidation of cyclopropylarenes
Wang, Yonghui,Tanko
, p. 2705 - 2711 (2007/10/03)
The chemistry of radical cations generated via the oxidation of several cyclopropylarenes with ceric(IV) ammonium nitrate in CH3CN-CH3OH is reported. For cyclopropylbenzene, the major product is 1-phenylpropane-1,3-diyl dinitrate, arising from ring opening of the cyclopropylbenzene radical cation. Experiments with 1-cyclopropyl-4-methylbenzene reveal that ring opening of cyclopropylbenzenes occurs substantially faster than side chain deprotonation. Cyclopropane ring opened products are also formed in the oxidation of 1- and 2-cyclopropylnaphthalenes. For 9-cyclopropylanthracene however, ring opened products are not detected. Instead, all products arising from this reaction are attributable to reaction of nucleophiles with the aromatic ring. Overall, these results confirm and extend earlier observations pertaining to the chemistry of cyclopropylarene radical cations. General principles associated with the use of cyclopropyl groups as "probes" for radical cation intermediates, and general principles governing radical ion ring openings are discussed.
Direct Observation of an Intermediate in the Oxygen Atom Rearrangement of 2-Cyclopropylnitrobenzene in a Strong Acid
Ohwada, Tomohiko,Kasuga, Mitsugu,Shudo, Koichi
, p. 2717 - 2719 (2007/10/02)
Direct spectroscopic observation revealed the formation of the 1,3-dihydro-3-ethyl-1-oxo-2,1-benzoxazolyl cation (3) from 2-cyclopropylnitrobenzene (1) in trifluoromethanesulfonic acid.This observation provided experimental evidence for the involvement of
Electrophilic Aromatic Nitration in the Gas Phase
Attina, Marina,Cacace, Fulvio,Yanez, Manuel
, p. 5092 - 5097 (2007/10/02)
Aromatic nitration by MeO+(H)NO2, in essence nitronium ion solvated by one methanol molecule, has been studied in the gas phase by using an integrated approach, based on the coordinate application of ICR, Cl, and CID mass spetrometric methods with a highly complementary radiolytic technique.The latter can be used in gases at atmospheric pressure and allows direct evaluation of key mechanistic features, in particular of substrate and positional selectivity.The results resolve early discrepancies between gas-phase and liquid-phase studies, characterizing the reaction as a typical, well-behaved electrophilic substitution of moderate selectivity.The date from the gas-phase nitration of ten monosubstituted benzenes fit a Hammett's type linear plot, characterized by a ρ value of -3.87.The correlation does not extend to highly activated substrates, such as anisole and mesitylene, since the nitration rate tends to a limiting value that cannot be increased by further enhancing the activation of the substrate, exactly as in "encounter-rate" nitrations occurring in solution.The mechanism and the energetics of the gas-phase nitration have been investigated, and the relative stability of the charged intermediates involved, in particular of the isomeric protonated nitrobenzenes, has been estimated by theoretical approaches at two different levels, using STO-3G minimal basis and 4-31G split-valence basis sets.
