5337-03-1Relevant articles and documents
Oxidation of Primary Alcohols and Aldehydes to Carboxylic Acids via Hydrogen Atom Transfer
Tan, Wen-Yun,Lu, Yi,Zhao, Jing-Feng,Chen, Wen,Zhang, Hongbin
supporting information, p. 6648 - 6653 (2021/09/08)
The oxidation of primary alcohols and aldehydes to the corresponding carboxylic acids is a fundamental reaction in organic synthesis. In this paper, we report a new chemoselective process for the oxidation of primary alcohols and aldehydes. This metal-free reaction features a new oxidant, an easy to handle procedure, high isolated yields, and good to excellent functional group tolerance even in the presence of vulnerable secondary alcohols and tert-butanesulfinamides.
Important intermediate tetrahydropyrane-4-formic acid preparation method
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Paragraph 0018-0052, (2019/01/13)
The invention discloses an important intermediate tetrahydropyrane-4-formic acid preparation method which comprises the following steps: mixing tetrahydropyrane-4-methanol with water, heating to 40 to50 DEG C, adding Mg-Ce-Mo-TiO2 compound oxide, evenly stirring, inflating O2, cooling to the room temperature after reaction finishes, filtering, performing reduced pressure distillation and recrystallizing to obtain tetrahydropyrane-4-formic acid. The synthesizing method disclosed by the invention has the advantages of simpleness in operation, mild condition, fewer byproducts, high product purity and higher product yield.
SUBSTITUTED AZASPIRO(4.5)DECANE DERIVATIVES
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Page/Page column 89, (2016/02/10)
The invention relates to substituted spirocyclic cyclohexane derivatives which have an affinity for the μ opioid receptor and/or the ORL1 receptor, processes for the preparation thereof, medicaments containing these compounds and the use of these compounds for the preparation of medicaments.
4-substituted or unsubstituted tetrahydropyran-4-carboxylic acid or its ester compound compd.
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Paragraph 0076, (2016/12/16)
A process for producing a 4-(un)substituted tetrahydropyran-4-carboxylic acid compound or an ester compound thereof which are represented by the formula (1): (1) (wherein R represents hydrogen or a hydrocarbon group; R represents hydrogen or an optionally substituted hydrocarbon group; and R represents hydrogen or a hydrocarbon group), characterized by reacting a 4-(un)substituted 4-cyanotetrahydropyran compound represented by the formula (2): (2) (wherein R and R are the same as defined above) with water or an alcohol which are represented by the formula (3): ROH (3) (wherein R is the same as defined above) in the presence of an acid or base.
Compounds with cardiac myosin activating function and pharmaceutical composition containing the same for treating or preventing heart failure
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Paragraph 1324-1328, (2016/10/07)
Disclosed are a compound having cardiotonic activity and a pharmaceutical composition containing the same, and the composition containing the compound, according to the present invention, is useful for preventing and treating heart failure.COPYRIGHT KIPO 2016
Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series
Liu, Longbin,Norman, Mark H.,Lee, Matthew,Xi, Ning,Siegmund, Aaron,Boezio, Alessandro A.,Booker, Shon,Choquette, Debbie,D'Angelo, Noel D.,Germain, Julie,Yang, Kevin,Yang, Yajing,Zhang, Yihong,Bellon, Steven F.,Whittington, Douglas A.,Harmange, Jean-Christophe,Dominguez, Celia,Kim, Tae-Seong,Dussault, Isabelle
experimental part, p. 1868 - 1897 (2012/05/04)
As part of our effort toward developing an effective therapeutic agent for c-Met-dependent tumors, a pyrazolone-based class II c-Met inhibitor, N-(4-((6,7-dimethoxyquinolin-4-yl)oxy)-3-fluorophenyl)-1,5-dimethyl-3-oxo-2- phenyl-2,3-dihydro-1H-pyrazole-4-c
2-OXO-2- (2-PHENYL-5,6,7,8-TETRAHYDRO-INDOLIZIN-3-YL) -ACETAMIDE DERIVATIVES AND RELATED COMPOUNDS AS ANTIFUNGAL AGENTS
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Page/Page column 14, (2011/02/15)
The invention provides compounds of formula (I), and pharmaceutically and agriculturally acceptable salts thereof: wherein: R1, R2, R3, R4, R5, R6, R7, R8, A1, L1 and n are as defined herein. These compounds and their pharmaceutically acceptable salts are useful in the manufacture of medicaments for use in the prevention or treatment of a fungal disease. Compounds of formula (I), and agriculturally acceptable salts thereof, may also be used as agricultural fungicides.
Structure-activity relationships of cycloalkylamide derivatives as inhibitors of the soluble epoxide hydrolase
Kim, In-Hae,Park, Yong-Kyu,Hammock, Bruce D.,Nishi, Kosuke
experimental part, p. 1752 - 1761 (2011/05/05)
Structure-activity relationships of cycloalkylamide compounds as inhibitors of human sEH were investigated. When the left side of amide function was modified by a variety of cycloalkanes, at least a C6 like cyclohexane was necessary to yield reasonable inhibition potency on the target enzyme. In compounds with a smaller cycloalkane or with a polar group on the left side of amide function, no inhibition was observed. On the other hand, increased hydrophobicity dramatically improved inhibition potency. Especially, a tetrahydronaphthalene (20) effectively increased the potency. When a series of alkyl or aryl derivatives of cycloalkylamide were investigated to continuously optimize the right side of the amide pharmacophore, a benzyl moiety functionalized with a polar group produced highly potent inhibition. A nonsubstituted benzyl, alkyl, aryl, or biaryl structure present on the right side of the cycloalkylamide function induced a big decrease in inhibition potency. Also, the resulting potent cycloalkylamide (32) showed reasonable physical properties.
AKT INHIBITORS
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Page/Page column 100, (2011/05/06)
The present invention provides AKT inhibitors of the formula: Formula I The present invention also provides pharmaceutical compositions comprising compounds of Formula I, uses of compounds of Formula I and method of using compounds of Formula I.
Modulation on C- and N-terminal moieties of a series of potent and selective linear tachykinin NK2 receptor antagonists
Gensini, Martina,Altamura, Maria,Dimoulas, Tula,Fedi, Valentina,Giannotti, Danilo,Giuliani, Sandro,Guidi, Antonio,Harmat, Nicholas J. S.,Meini, Stefania,Nannicini, Rossano,Pasqui, Franco,Tramontana, Manuela,Triolo, Antonio,Maggi, Carlo Alberto
scheme or table, p. 65 - 78 (2010/11/16)
Herein we describe the synthesis of a series of new potent tachykinin NK2 receptor antagonists by the modulation of the Cand N-terminal moieties of ibodutant (MEN 15596, 1). The Nterminal benzo[b]thiophene ring was replaced by different substituted naphthalenes and benzofurans, while further modifications were evaluated at the C-terminal tetrahydropyran moiety. Most compounds demonstrated a high affinity for the human NK2 receptor and high in vitro antagonist potency, indicating that a wide range of substituents at both termini can be incorporated in the molecule without detrimental effects on the interactions with the NK2 receptor. Selected compounds were tested in vivo confirming their activity as NK2 antagonists. In particular, after both iv and id administration to guinea pig, compound 61b was able to antagonize NK2-induced colonic contractions with a potency and duration-of-action fully comparable to the reference compound 1 (MEN 15596, ibodutant).