18621-17-5Relevant articles and documents
Indirect reduction of CO2and recycling of polymers by manganese-catalyzed transfer hydrogenation of amides, carbamates, urea derivatives, and polyurethanes
Liu, Xin,Werner, Thomas
, p. 10590 - 10597 (2021/08/20)
The reduction of polar bonds, in particular carbonyl groups, is of fundamental importance in organic chemistry and biology. Herein, we report a manganese pincer complex as a versatile catalyst for the transfer hydrogenation of amides, carbamates, urea derivatives, and even polyurethanes leading to the corresponding alcohols, amines, and methanol as products. Since these compound classes can be prepared using CO2as a C1 building block the reported reaction represents an approach to the indirect reduction of CO2. Notably, these are the first examples on the reduction of carbamates and urea derivatives as well as on the C-N bond cleavage in amides by transfer hydrogenation. The general applicability of this methodology is highlighted by the successful reduction of 12 urea derivatives, 26 carbamates and 11 amides. The corresponding amines, alcohols and methanol were obtained in good to excellent yields up to 97%. Furthermore, polyurethanes were successfully converted which represents a viable strategy towards a circular economy. Based on control experiments and the observed intermediates a feasible mechanism is proposed.
Selective Deprotection of the Diphenylmethylsilyl (DPMS) Hydroxyl Protecting Group under Environmentally Responsible, Aqueous Conditions
Akporji, Nnamdi,Lieberman, Josh,Maser, Michael,Yoshimura, Masahiko,Boskovic, Zarko,Lipshutz, Bruce H.
, p. 5743 - 5747 (2019/11/11)
Two new methods for selective deprotection of diphenylmethylsilyl (DPMS) ethers are described. Unmasking can be achieved with either catalytic amounts of perfluoro-1-butanesulfonyl fluoride (a SuFEx reagent) under mild, aqueous micellar conditions, or using stoichiometric amounts of 18-crown-6 ether in aqueous ethanol.
TAU-PROTEIN TARGETING PROTACS AND ASSOCIATED METHODS OF USE
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Paragraph 1022, (2018/05/24)
The present disclosure relates to bifunctional compounds, which find utility as modulators of tau protein. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a VHL or cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds tau protein, such that tau protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of tau. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of tau protein. Diseases or disorders that result from aggregation or accumulation of tau protein are treated or prevented with compounds and compositions of the present disclosure.
Synthesis of Novel Hybrid 4 H -Pyran-lipoic and 4 H -Pyran-azetidine Derivatives
Hernández-Borja, Fernando,Contreras, Leticia,López, Julio,Alcaraz, Yolanda,Cruz, David,Estrada-Soto, Samuel,Delgado, Francisco,Vázquez, Miguel A.
, p. 1020 - 1026 (2017/11/29)
In this study, a molecular hybridization strategy was used to design and synthesize two novel series of hybrid compounds: 4 H -pyran-lipoic and 4 H -pyran-azetidine, employing ammonium hydroxide and involving the participation of aldehydes, malononitrile, and compounds derived from β-ketoesters to obtain the products with good yields.
Preparation method of N-diphenylmethyl-3-hydroxyazetidine
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Paragraph 0022; 0023; 0024; 0025; 0026, (2017/05/16)
The invention relates to a preparation method of azelnidipine intermediate N-(diphenylmethyl)-3-hydroxyazetidine. The preparation method is disclosed based improvement of a conventional method. According to the preparation method, an alkali is added into a reaction system, so that reaction time is shortened from 48h to 16h or less, the reaction time is shortened greatly, and energy consumption is reduced; yield can be maintained to be 83 to 88%, and product purity is increased to be higher than 99.9% via effective adjustment of reaction temperature and appropriate postprocessing, and the preparation method is extremely suitable for industrialized production.
JAK INHIBITOR
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Paragraph 0289; 0290; 0291, (2017/12/15)
The present invention discloses a series of JAK inhibitors, and particularly discloses a compound of formula (I) or a pharmaceutically acceptable salt thereof and the use thereof in preparation of drugs for treating diseases related to JAK.
9-AMINOMETHYL SUBSTITUTED TETRACYCLINE COMPOUND
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Paragraph 0160-0162, (2014/06/24)
The present invention relates to 9-aminomethyl substituted tetracycline compounds represented by formula (I), or pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, as well as a method for preparing these compounds and a pharmaceutical composition comprising the same. The present invention relates also to a use of these compounds in the preparation of a medicament for the treatment and/or prophylaxis of tetracycline drug-sensitive disease. wherein, R2a, R2b, R3, R4a, R4b, R5, R6a, R6b, R7, R8, R9a, R9b, R10, R11, R12, R13a and R13b are each independently as defined in the description.
PROCESSES AND INTERMEDIATES FOR MAKING A JAK INHIBITOR
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Paragraph 0155, (2014/09/29)
This invention relates to processes and intermediates for making {1-{1-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile, useful in the treatment of diseases related to the activity of Janus kinases (JAK) including inflammatory disorders, autoimmune disorders, cancer, and other diseases.
Acylazetine as a dienophile in bioorthogonal inverse electron-demand Diels-Alder ligation
Engelsma, Sander B.,Willems, Lianne I.,Van Paaschen, Claudia E.,Van Kasteren, Sander I.,Van Der Marel, Gijsbert A.,Overkleeft, Herman S.,Filippov, Dmitri V.
supporting information, p. 2744 - 2747 (2014/06/09)
A new bioorthogonal N-acylazetine tag, suitable for tetrazine mediated inverse electron-demand Diels-Alder conjugation, is developed. The tag is small and achiral. We demonstrate the usefulness of N-acylazetine-tetrazine based bioorthogonal chemistry in two-step activity-based protein profiling. The performance of the new tetrazinophile in the labeling of catalytically active proteasome subunits was comparable to that of the more sterically demanding norbornene tag.
9-AMINOMETHYL SUBSTITUTED TETRACYCLINE COMPOUNDS
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Page/Page column, (2014/07/08)
The present invention relates to 9-aminomethyl substituted tetracycline compounds represented by formula (I), or pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, as well as a method for preparing these compounds and a pharmaceutical composition comprising the same. The present invention relates also to a use of these compounds in the preparation of a medicament for the treatment and/or prophylaxis of tetracycline drug-sensitive disease. wherein, R2a, R2b, R3, R4a, R4b, R5, R6a, R6b, R7, R8, R9a, R9b, R10, R11, R12, R13a and R13b are each independently as defined in the description.
