40696-22-8Relevant articles and documents
ION CHANNEL ANTAGONISTS/BLOCKERS AND USES THEREOF
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Page/Page column 22; 24; 49, (2021/06/22)
Provided are ion channel antagonists/blockers and uses thereof. Specifically, it provides the compounds of formula (I) or pharmaceutically acceptable salts, stereoisomers, solvates or prodrugs, preparation method therefor and application thereof. Definition of each group in the formula can be found in the specification for details. Provided is also pharmaceutical composition useful for treatment of heart disease and other ion channel related diseases.
Base-Induced Cyclisation of ortho -Substituted 2-Phenyloxazolines to Give 3-Aminobenzofurans and Related Heterocycles
Aitken, R. Alan,Harper, Andrew D,Slawin, Alexandra M. Z.
supporting information, p. 1738 - 1742 (2017/10/06)
Treatment of ortho -benzyloxyphenyloxazolines with butyllithium and potassium tert -butoxide results in cyclisation with ring opening of the oxazoline to give 2-aryl-3-aminobenzofurans. The reaction also occurs with the corresponding benzylthio and benzylamino compounds to give benzothiophenes and indoles, respectively. Use of an ortho -allyloxyphenyloxazoline gives the corresponding 2-vinylbenzofuran, while both α-methylbenzyloxy and benzylsulfonyl compounds form stable spirooxazolidine products. The X-ray structure of an aminobenzothiophene product has been determined.
Thienopyrimidinone Based Sirtuin-2 (SIRT2)-Selective Inhibitors Bind in the Ligand Induced Selectivity Pocket
Sundriyal, Sandeep,Moniot, Sébastien,Mahmud, Zimam,Yao, Shang,Di Fruscia, Paolo,Reynolds, Christopher R.,Dexter, David T.,Sternberg, Michael J. E.,Lam, Eric W.-F.,Steegborn, Clemens,Fuchter, Matthew J.
, p. 1928 - 1945 (2017/03/17)
Sirtuins (SIRTs) are NAD-dependent deacylases, known to be involved in a variety of pathophysiological processes and thus remain promising therapeutic targets for further validation. Previously, we reported a novel thienopyrimidinone SIRT2 inhibitor with good potency and excellent selectivity for SIRT2. Herein, we report an extensive SAR study of this chemical series and identify the key pharmacophoric elements and physiochemical properties that underpin the excellent activity observed. New analogues have been identified with submicromolar SIRT2 inhibtory activity and good to excellent SIRT2 subtype-selectivity. Importantly, we report a cocrystal structure of one of our compounds (29c) bound to SIRT2. This reveals our series to induce the formation of a previously reported selectivity pocket but to bind in an inverted fashion to what might be intuitively expected. We believe these findings will contribute significantly to an understanding of the mechanism of action of SIRT2 inhibitors and to the identification of refined, second generation inhibitors.
Palladium-catalyzed amination of chloromethylnaphthalene and chloromethylanthracene derivatives with various amines
Zhang, Sheng,Wang, Yi,Feng, Xiujuan,Bao, Ming
supporting information; experimental part, p. 5492 - 5495 (2012/05/20)
Palladium-catalyzed amination of chloromethylnaphthalene and chloromethylanthracene derivatives to produce naphthylamines and anthrylamines in satisfactory to good yields has been developed. The unprecedented amination reactions proceeded smoothly under mild conditions in the presence of Pd(PPh3)4 as a catalyst.
A simple method for deprotection of tert-butyldimethylsilyl ethers by using stannous chloride under microwave irradiation
Jadhav, Vinod H.,Borate, Hanumant B.,Wakharkar, Radhika D.
, p. 322 - 324 (2007/10/03)
A facile regeneration of hydroxy compounds from their tert- butyldimethylsilyl ethers in presence of stannous chloride under solvent free conditions using domestic microwave oven has been performed efficiently in a short period (5-6 min). The conversion using stannous chloride in ethanol or water for comparison of the efficiency has been described. The generality of the transformation has been confirmed by several examples.
O-arylmethyl-N-(thio)acylhydroxylamines
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, (2008/06/13)
The invention relates to a compound selected from those of formula (I): STR1 in which Ar, X, R 1 and R 2 are as defined in the description and a medicinal product containing the same in order to treat a disorder of the melatoninergic system.
Spirans. Part 13. The Synthesis and Orientation of Spirans related to Abel's Ketone (Naphthofuran-2(1H)-spiro-1'(2'H)-naphthalen-2'-one)
Dean, Francis M.,Herbin, G. Antonio,Matkin, David A.,Price, Anthony W.,Robinson, Malcolm L.
, p. 1986 - 1993 (2007/10/02)
The aryl substituents in the stereoisomers (2) and (3) of 1-phenylnaphthofuran-2(1H)-spiro-1'(2'H)-naphthalen-2'-one are subject to hindered rotation by an energy barrier of ca. 15 kcal mol-1.If the phenyl substituent carries an ortho substituent, however, rotation is prevented at temperatures up to 60 deg C (the highest examined): only one rotamer is obtainable (the other is too crowded) and it has the ortho-substituent cisoid with respect to the triarylmethine proton. The temperature-variable broadening of the signals from the protons of the aryl substituent serves to identify these in the 1H n.m.r. spectra.Some other resonances can be regularly identified by combinations of coupling constants, double-irradiation experiments, and shifts induced by using benzene instead of trichloromethane as sovent, but the only one of value for determining the configuration at the triarylmethine centre is that already known, i.e. the upfield shift in the resonance of the vinylic (3') proton caused by the aryl substituent when this lies immediately below it.A less precise but more general test of configuration is afforded by the mutual shielding of the aryl substituent and ring E when these are in adjacent planes. Methods of preparation are given for several related spirans, especially those containing the spiro-1'(4'H)-naphthalen-4'-one nucleus, and n.m.r. methods used to establish the configurations.
