- Ru-catalyzed mechanochemical asymmetric transfer hydrogenations in aqueous media using chitosan as chirality source
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As the demand for sustainable methods increases, synthetic chemistry is focusing on the application of environmentally benign methods, such as fast reactions induced by alternative energy transmission. Chitosan is a chiral biopolymer of natural origin, which can be used in asymmetric catalysis. The application of Ru-chitosan complexes along with the mechanochemical activation may open great opportunities for sustainable preparation of optically pure alcohols. In the present study, we optimized the mechanochemical asymmetric transfer hydrogenation of 4-chromanone, carried out in a mixing mill. The reaction was catalyzed by the in situ formed Ru-chitosan complex, applying HCOONa as the hydrogen donor in aqueous media. We examined the mechanical effects of different grinding media sizes, then explored the scope of the system using 24 prochiral ketones, which ranged from hetero- and carbocyclic ketones to acetophenone derivatives. In most of the cases, the reactions were successfully scaled up to 1 mmol and the products were isolated in good yields and outstanding enantioselectivities. Our present study is a significant step forward to the development of environmentally benign and sustainable enantioselective processes, as the alternative activation method provided optically enriched alcohols using a biodegradable chirality source in aqueous media.
- Kolcsár, Vanessza Judit,Sz?ll?si, Gy?rgy
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- Immunomodulatory compound, compositions and application thereof
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The invention discloses an amide compound with a novel structure or a stereoisomer of the amide compound or a stereoisomer mixture of the amide compound and pharmaceutically acceptable salts of the amide compound, and application of the compound in preparation of drugs for treating diseases, obstacles or symptoms which benefit from inhibition of PD1 or PD-L1 activity. The compound disclosed by the invention shows very strong PD-1/PD-L1 blocking activity, and can reverse T cell functions inhibited by PD-L1 at the same time. Meanwhile, the compound provided by the invention can activate an NFAT signal channel caused by PD-1/PD-L1 combination, can be absorbed by oral administration, and has good pharmacokinetic properties. Therefore, the compound of the present invention can be used in the treatment of diseases, disorders or conditions that benefit from the inhibition of the PD1 or PD-L1 activity, including infectious diseases, immune diseases, inflammatory diseases and cancers, alone or used in combination with other drugs.
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Paragraph 0660-0662
(2021/05/19)
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- Asymmetric Magnesium-Catalyzed Hydroboration by Metal-Ligand Cooperative Catalysis
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Asymmetric catalysis with readily available, cheap, and non-toxic alkaline earth metal catalysts represents a sustainable alternative to conventional synthesis methodologies. In this context, we describe the development of a first MgII-catalyzed enantioselective hydroboration providing the products with excellent yields and enantioselectivities. NMR spectroscopy studies and DFT calculations provide insights into the reaction mechanism and the origin of the enantioselectivity which can be explained by a metal-ligand cooperative catalysis pathway involving a non-innocent ligand.
- Falconnet, Alban,Magre, Marc,Maity, Bholanath,Cavallo, Luigi,Rueping, Magnus
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supporting information
p. 17567 - 17571
(2019/11/13)
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- COMPOUNDS USEFUL AS IMMUNOMODULATORS
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The present disclosure generally relates to compounds useful as immunomodulators. Provided herein are compounds, compositions comprising such compounds, and methods of their use. The disclosure further pertains to pharmaceutical compositions comprising at least one compound according to the disclosure that are useful for the treatment of various diseases, including cancer and infectious diseases.
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Page/Page column 33-34
(2019/09/18)
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- Novel phenyl propionic acid compound as GPR40 agonist
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The present invention relates to a novel phenyl propionic acid derivative having the structure of chemical formula (I) and having a GPR40 agonist action that shows an inhibitory effect on the elevation of blood glucose level through promoting insulin secretion according to glucose tolerance; a preparation method of the same; and a pharmaceutical composition comprising the same as an active ingredient for preventing or treating metabolic diseases. In the chemical formula (I), groups of R_1-R_4, and X are as defined in claim 1.COPYRIGHT KIPO 2018
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Paragraph 0149-0151
(2018/09/30)
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- PD-1/PD-L1 INHIBITORS
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Compounds according to formula (I), methods of using said compounds singly or in combination with additional agents and compositions of said compounds for the treatment of cancer are disclosed.
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Page/Page column 207
(2018/11/22)
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- SELECTIVE HETEROCYCLIC SPHINGOSINE 1 PHOSPHATE RECEPTOR MODULATORS
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Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds is provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.
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Paragraph 0254; 0255
(2015/11/18)
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- NEW INDANYLOXYDIHYDROBENZOFURANYLACETIC ACID DERIVATIVES AND THEIR USE AS GPR40 RECEPTOR AGONISTS
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The present invention relates to compounds of general formula (I), wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
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Page/Page column 95
(2013/10/21)
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- CARBOXYLIC ACID COMPOUND
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To find a therapeutic agent and/or a preventive agent for diabetes mellitus or the like having excellent activity and safety. A compound represented by the following general formula (I), or a pharmacologically acceptable salt thereof. In the formula, X re
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Page/Page column 74
(2011/04/14)
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