3187-32-4Relevant academic research and scientific papers
NON-LYSOSOMAL GLUCOSYLCERAMIDASE INHIBITORS AND USES THEREOF
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Paragraph 00185, (2020/12/01)
The invention provides compounds for inhibiting glucosylceramidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds.
A phosphine-free iron complex-catalyzed synthesis of cycloalkanes: Via the borrowing hydrogen strategy
Bettoni, Léo,Gaillard, Sylvain,Renaud, Jean-Luc
supporting information, p. 12909 - 12912 (2020/11/07)
Herein we report a diaminocyclopentadienone iron tricarbonyl complex catalyzed synthesis of substituted cyclopentane, cyclohexane and cycloheptane compounds using the borrowing hydrogen strategy in the presence of various substituted primary and secondary 1,n diols as alkylating reagents. Deuterium labeling experiments confirm that the diols were the hydride source in this cascade process. This journal is
Stereoselective synthesis of alicyclic ketones: A hydrogen borrowing approach
Armstrong, Roly J.,Akhtar, Wasim M.,Frost, James R.,Christensen, Kirsten E.,Stevenson, Neil G.,Donohoe, Timothy J.
supporting information, (2019/11/13)
A highly diastereoselective annulation strategy for the synthesis of alicyclic ketones from diols and pentamethylacetophenone is described. This process is mediated by a commercially available iridium(III) catalyst, and provides efficient access to a wide range of cyclopentane and cyclohexane products with high levels of stereoselectivity. The origins of diastereoselectivity in the annulation reaction have been explored by a series of control experiments, which provides an explanation for how each stereocentre around the newly forged ring is controlled.
Stereoselective Synthesis of Cyclohexanes via an Iridium Catalyzed (5 + 1) Annulation Strategy
Akhtar, Wasim M.,Armstrong, Roly J.,Frost, James R.,Stevenson, Neil G.,Donohoe, Timothy J.
supporting information, p. 11916 - 11920 (2018/09/27)
An iridium catalyzed method for the synthesis of functionalized cyclohexanes from methyl ketones and 1,5-diols is described. This process operates by two sequential hydrogen borrowing reactions, providing direct access to multisubstituted cyclic products with high levels of stereocontrol. This methodology represents a novel (5 + 1) strategy for the stereoselective construction of the cyclohexane core.
Iron(II) pincer-catalyzed synthesis of lactones and lactams through a versatile dehydrogenative domino sequence
Pea-Lpez, Miguel,Neumann, Helfried,Beller, Matthias
, p. 865 - 871 (2015/03/14)
The synthesis of lactones and lactams by using iron(II) pincer-catalyzed dehydrogenative methodology was developed. Starting from 1,n-diols or 1,n-amino alcohols, this domino transformation takes place through initial dehydrogenation of the substrates, subsequent intramolecular cyclization, and final oxidation to afford the desired products in good yields. The ability to access heterocycles of different sizes makes this protocol especially versatile, in which two consecutive oxidation reactions are performed without requiring an external oxidant. In this paper, we report the application of the Fe-MACHO-BH complex [carbonylhydrido(tetrahydroborato)[bis(2-diisopropylphosphinoethyl)amino]iron(II)] in this atom-efficient and environmentally benign process, for which molecular hydrogen is formed as the only stoichiometric side product. Just a little pinch: The iron(II) pincer-catalyzed synthesis of lactones and lactams from easily available 1,n-diols and 1,n-amino alcohols is explored. The use of a nontoxic metal as well as the generation of molecular hydrogen as the only stoichiometric byproduct makes this method a highly atom-efficient and environmentally benign process.
APOPTOSIS INDUCERS
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Paragraph 00290; 00291, (2014/01/08)
This invention comprises novel compounds which inhibit the activity of anti-apoptotic Bcl-2 family protein members, compositions containing the compounds and methods of treating diseases involving a defect in apoptosis, such as, for example, in the treatment of cancer.
Four nucleophilic additions to alkenynedioic acid derivatives in tandem; Efficient one-pot synthesis of bicyclo[4.2.0]octenols
Hata, Takeshi,Imade, Haduki,Urabe, Hirokazu
supporting information; scheme or table, p. 2450 - 2453 (2012/07/27)
When alkenynedioic acid derivatives were treated with a Grignard reagent, tandem cyclization and the incorporation of two molecules of the Grignard reagent occurred to give stereodefined bicyclo[4.2.0]octenols via four nucleophilic additions.
SUBSTITUTED AMINOTHIAZOLE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE
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Page/Page column 71, (2010/04/06)
Substituted aminothiazole derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted aminothiazole, and methods of use in treating human or animal disorders. The compounds may be useful as inhibitors of action of AgRP on a melanocortin receptor and thus may be useful for the management, treatment, control, or the adjunct treatment of diseases which may be responsive to the modulation of melanocortin receptors including obesity-related disorders.
Alkylsubstituted Cyclopentanones via Hydrocarbonylating Cyclization of 1,4-Pentadiene Systems Mediated by Metal Carbonyls
Eilbracht, Peter,Acker, Michael,Totzauer, Walter
, p. 238 - 242 (2007/10/02)
3,3-Dialkyl-1,4-pentadienes 8 under the influence of metal carbonyls can be converted to unsymmetrically substituted cyclopentanones 9 by hydrocarbonylating cyclization with carbon monoxide and hydrogen or water.Starting from 1,1-divinylcycloalkanes of type 8 this method can also be used for the synthesis of spirocyclopentanones.The yields of cyclic ketones with the here used dienes are markedly better than with the unsubstituted 1,4-pentadiene itself.
