41374-66-7Relevant academic research and scientific papers
Discovery and optimization of substituted oxalamides as novel heme-displacing IDO1 inhibitors
Steeneck, Christoph,Kinzel, Olaf,Anderhub, Simon,Hornberger, Martin,Pinto, Sheena,Morschhaeuser, Barbara,Albers, Michael,Sonnek, Christina,Czekańska, Marta,Hoffmann, Thomas
supporting information, (2021/01/18)
Since the advent of antibody checkpoint inhibitors as highly efficient drugs for cancer treatment, the development of immunomodulating small molecules in oncology has gained great attention. Drug candidates targeting IDO1, a key enzyme in tryptophan metab
Asymmetric Transfer Hydrogenation of α-Keto Amides; Highly Enantioselective Formation of Malic Acid Diamides and α-Hydroxyamides
Gediya, Shweta K.,Vyas, Vijyesh K.,Clarkson, Guy J.,Wills, Martin
supporting information, p. 7803 - 7807 (2021/10/20)
The asymmetric transfer hydrogenation (ATH) of α-keto-1,4-diamides using a tethered Ru/TsDPEN catalyst was achieved in high ee. Studies on derivatives identified the structural elements which lead to the highest enantioselectivities in the products. The α-keto-amide reduction products have been converted to a range of synthetically valuable derivatives.
POLYCYCLIC COMPOUND ACTING AS IDO INHIBITOR AND/OR IDO-HDAC DUAL INHIBITOR
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Paragraph 0245-0246, (2020/08/09)
The present invention provides polycyclic compounds as IDO inhibitors and/or dual inhibitors of IDO-HDAC. Specifically, the present invention provides compounds represented by the following formula (I), wherein each group is defined as described in the specification. The compounds have IDO inhibitory activity or IDO-HDAC dual inhibitory activity and can be used for preventing or treating diseases associated with IDO and/or IDO-HDAC activity or expression levels. At the same time, the compounds of the present invention can be combined with an antitumor antibody such as PD-1 and PD-L1, and such a combination can greatly increase the antitumor response rate of the antibody and broaden the types of tumors to be treated.
Copper-Catalysed (Diacetoxyiodo)benzene-Promoted Aerobic Esterification Reaction: Synthesis of Oxamates from Acetoacetamides
Zhang, Zhiguo,Gao, Xiaolong,Yu, Haifeng,Zhang, Guisheng,Liu, Jianming
supporting information, p. 3406 - 3411 (2018/07/31)
A copper-catalysed (diacetoxyiodo)benzene-promoted aerobic esterification reaction of acetoacetamides was developed for the synthesis of oxamates, which are useful precursors in synthetic organic chemistry. This practical and mild synthetic approach proceeded at 25 °C under open-air conditions and afforded methyl 2-oxo-2-(phenylamino)acetates in good to excellent yields combined with C?C σ-bond cleavage and formal oxidative C?H bond functionalization. A mechanism is proposed. (Figure presented.).
Hypervalent iodine(III)-promoted: N -incorporation into N -aryl vinylogous carbamates to quinoxaline diesters: Access to 1,4,5,8-tetraazaphenanthrene
Sagar,Vidaycharan, Shinde,Shinde, Anand H.,Sharada, Duddu S.
supporting information, p. 4018 - 4022 (2016/06/14)
A novel oxidative N-incorporation strategy for synthesis of quinoxaline diesters under metal-free conditions is described for the first time. The mild reaction conditions allow for this transformation via the formation of two C(sp2)-N bonds utilizing cheaply available NaN3 as the N-atom source. N-Aryl vinylogous carbamates in this study undergo azidation at enamino C(sp2)-H selectively. The robustness of this strategy is further demonstrated by the synthesis of a valuable 1,4,5,8-tetraazaphenanthrene derivative using a mild and convenient approach.
Synthesis of N -arylisatins by the reaction of arynes with methyl 2-Oxo-2-(arylamino)acetates
Rogness, Donald C.,Larock, Richard C.
experimental part, p. 4980 - 4986 (2011/08/06)
N-Arylisatins are efficiently prepared by the reaction of 2-oxo-2-(arylamino)acetates and arynes under mild reaction conditions
Synthesis of methyl N-aryl oxamate using soluble polymer support
Yang, Guichun,Zhang, Haiqing,Huang, Yanling,Chen, Zuxing
, p. 611 - 619 (2007/10/03)
A variety of methyl N-aryl oxamates were synthesized using poly(ethylene glycol) (PEG) as a soluble polymer support and a monoproctection group with excellent yields. Copyright Taylor & Francis Group, LLC.
NOVEL ETHYLENEDIAMINE DERIVATIVES
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Page/Page column 59-60, (2010/02/14)
A compound represented by the following formula (1):Q-Q-T-N(R)-Q-N(R)-T-Q [wherein, R1 and R2 are hydrogen atoms or the like; Q1 is a saturated or unsaturated, 5- or 6- membered cyclic hydrocarbon group which may have a substituent, or the like; Q2 is a single bond or the like; Q3 represents the following group: -C(R3a)(R4a)-{C(R3b)(R4b)}m1-{C(R3c)(R4c)}m2-{C(R3d)(R4d)}m3-{C(R3e)(R4e)}m4-C(R3f)(R4f)- (in which, R3a to R4e represent hydrogen or the like); T0 represents a carbonyl group or the like; and T1 represents -COCONR- or the like]; or salt thereof, solvate thereof, or N-oxide thereof. The compound is useful as a preventive and/or therapeutic agent for cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary infarction, pulmonary embolism, Buerger's disease, deep venous thrombosis, disseminated intravascular coagulation syndrome, thrombus formation after valve or joint replacement, thrombus formation and reocclusion after angioplasty, systemic inflammatory response syndrome (SIRS), multiple organ dysfunction syndrome (MODS), thrombus formation during extracorporeal circulation, or blood clotting upon blood drawing.
Reactivity of Carbamoyl Radicals. A New, General, Convenient Free-Radical Synthesis of Isocyanates from Monoamides of Oxalic Acid
Minisci, Francesco,Fontana, Francesca,Coppa, Fausta,Yan, Yong Ming
, p. 5430 - 5433 (2007/10/02)
A new, general, simple synthesis of isocyanates was developed by oxidation of monoamides of oxalix acid with peroxydisulfate catalyzed by Ag and Cu salts.The reaction was carried out in a two-phase system (water and an organic solvent), and it is suitable also for practical applications, due to the simple experimental conditions and the inexpensive as well as nontoxic reagents.The first example of homolytic intramolecular aromatic carbamoylation is also reported.
