10292-61-2Relevant academic research and scientific papers
Lewis Base-Promoted Ring-Opening 1,3-Dioxygenation of Unactivated Cyclopropanes Using a Hypervalent Iodine Reagent
Gieuw, Matthew H.,Ke, Zhihai,Yeung, Ying-Yeung
supporting information, p. 3782 - 3786 (2018/03/13)
A facile and effective system has been developed for the regio- and chemoselective ring-opening/electrophilic functionalization of cyclopropanes through C?C bond activation by [bis(trifluoroacetoxy)iodo]benzene with the aid of the Lewis basic promoter p-toluenesulfonamide. The p-toluenesulfonamide-promoted system works well for a wide range of cyclopropanes, resulting in the formation of 1,3-diol products in good yields and regioselectivity.
HCV POLYMERASE INHIBITORS
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Page/Page column 63, (2020/02/14)
The invention provides compounds of the formula:wherein B is a nucleobase selected from the groups (a) to (d):and the other variables are as defined in the claims, which are of use in the treatment or prophylaxis of hepatitis C virus infection, and related aspects.
Direct hydroxylation of benzene and aromatics with H2O2 catalyzed by a self-assembled iron complex: Evidence for a metal-based mechanism
Capocasa, Giorgio,Olivo, Giorgio,Barbieri, Alessia,Lanzalunga, Osvaldo,Di Stefano, Stefano
, p. 5677 - 5686 (2017/12/07)
An iminopyridine Fe(ii) complex, easily prepared in situ by self-assembly of cheap and commercially available starting materials (2-picolylaldehyde, 2-picolylamine, and Fe(OTf)2 in a 2 : 2 : 1 ratio), is shown to be an effective catalyst for the direct hydroxylation of aromatic rings with H2O2 under mild conditions. This catalyst shows a marked preference for aromatic ring hydroxylation over lateral chain oxidation, both in intramolecular and intermolecular competitions, as long as the arene is not too electron poor. The selectivity pattern of the reaction closely matches that of electrophilic aromatic substitutions, with phenol yields and positions dictated by the nature of the ring substituent (electron-donating or electron-withdrawing, ortho-para or meta-orienting). The oxidation mechanism has been investigated in detail, and the sum of the accumulated pieces of evidence, ranging from KIE to the use of radical scavengers, from substituent effects on intermolecular and intramolecular selectivity to rearrangement experiments, points to the predominance of a metal-based SEAr pathway, without a significant involvement of free diffusing radical pathways.
DIOXOLANE ANALOGUES OF URIDINE FOR THE TREATMENT OF CANCER
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Page/Page column 36, (2016/03/22)
The invention provides compounds of formula (I), wherein: R1 is OR11, or NR5R5'; R2 is H or F; R5 is H, C1-C6alkyl, OH, C(=O)R6, O(C=O)R6 or O(C=O)OR6; R5′ is H or C1-C6alkyl; R6 is C1-C6alkyl or C3-C7cycloalkyl; R13 is H, phenyl, pyridyl, benzyl, indolyl or naphthyl wherein the phenyl, pyridyl, benzyl, indolyl and naphthyl is optionally substituted with 1, 2 or 3 R22; and the other variables are as defined in the claims, which are of use in the treatment of cancer, and related aspects.
HCV POLYMERASE INHIBITORS
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Page/Page column 53, (2015/03/28)
The invention provides compounds of the formula:(I) wherein B is a nucleobase selected from the groups (a) to (d) and the other variables are as defined in the claims, which are of use in the treatment or prophylaxis of hepatitis C virus infection, and related aspects.
HCV POLYMERASE INHIBITORS
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Page/Page column 55, (2015/05/05)
The invention provides compounds of the formula (I) wherein B is a nucleobase selected from the groups (a) to (d): and the other variables are as defined in the claims, which are of use in the treatment or prophylaxis of hepatitis C virus infection, and related aspects.
PYRIMIDINE COMPOUNDS AS DELTA OPIOID RECEPTOR MODULATORS
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Page/Page column 55, (2011/05/08)
Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows:wherein R1, R2, R3, and L, A, and Ra are defined herein.
BENZIMIDAZOLE TRPV1 INHIBITORS
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Page/Page column 70, (2008/12/06)
The invention is directed to compounds of Formula (I): to pharmaceutical compositions containing such compounds and to methods of treatment using them.
Preparation, antimicrobial evaluation, and mutagenicity of [2- hydroxyaryl]-[1-methyl-5-nitro-1H-2-imidazolyl]methanols, [5-tert-butyl-2- methylaminophenyl]-[1-methyl-5-nitro-1H-2-imidazolyl] methanol, and [2- hydroxyaryl]-[1-methyl-5-nitro-1H-2-imidazolyl] ketones
Arredondo,Moreno-Manas,Pleixats,Palacin,Raga,Castello,Ortiz
, p. 1959 - 1968 (2007/10/03)
Efficient preparations of the titled compounds are described, their antimicrobial activity and mutagenic properties being evaluated. Some of the studied compounds are nonmutagenic and present a MIC as low as some of the usual standards in the field.
Electron transfer in P450 mechanisms. Microsomal metabolism of cyclopropylbenzene and p-cyclopropylanisole
Riley,Hanzlik
, p. 1 - 16 (2007/10/03)
The metabolism of cyclopropylbenzene (1a) and 4-cyclopropylanisole (1b) was studied using liver microsomal preparations from control, phenobarbital- and β-naphthoflavone treated rats. With all three types of microsomes 1a was metabolized by benzylic hydroxylation to give 1-phenylcyclopropanol and by aromatic hydroxylation at C-4; the former predominated by a factor of 2-4. BNF-induced microsomes also formed 2-cyclopropylphenol. No cyclopropyl ring-opened metabolites of 1a, including benzoic acid, were detected in any of the incubations. With PB-induced microsomes 1b underwent O-demethylation (90%) and benzylic hydroxylation; no other metabolites were detected. Progress curves for metabolism of 1a are markedly nonlinear after only limited conversion of substrate, suggesting the possibility that 1a, like other cyclopropyl compounds, could be a suicide substrate for one or more isozymes of P450. For both 1a and b, metabolite formation and enzyme inactivation can be explained by conventional P450 reaction mechanisms not involving electron abstraction.
