114746-70-2Relevant academic research and scientific papers
ARYLMETHYLENE HETEROCYCLIC COMPOUNDS AS KV1.3 POTASSIUM SHAKER CHANNEL BLOCKERS
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Paragraph 0327; 0328, (2021/04/17)
A compound of Formula (I) or a pharmaceutically acceptable salt thereof is described, wherein the substituents are as defined herein. Pharmaceutical compositions comprising the same and method of using the same are also described.
H-Phosphonate Synthesis and Biological Evaluation of an Immunomodulatory Phosphoglycolipid from Thermophilic Bacteria
Gan, Chin Heng,Hua, Kuo-Feng,Lam, Yulin,Li, Lan-Hui,Peng, Yi-Jen,Wei, Chih-Feng,Wijaya, Hadhi,Wu, Shih-Hsiung
supporting information, (2020/04/02)
The synthesis of a library of bacterial phosphoglycolipid, PGL-1, is described. Key features of the synthesis include regioselective esterification of the primary alcohol of the diacylglycerol moiety and an H-phosphonate method to install the phosphate in PGL-1 in comparison with earlier reported procedures. A representative set of PGL-1 analogues was prepared and evaluated for their biological activities. Results showed that the immunological activity of PGL-1 is dependent on the chain lengths of the fatty acids.
Electrochemical Oxidation of Alcohols and Aldehydes to Carboxylic Acids Catalyzed by 4-Acetamido-TEMPO: An Alternative to "anelli" and "pinnick" Oxidations
Rafiee, Mohammad,Konz, Zachary M.,Graaf, Matthew D.,Koolman, Hannes F.,Stahl, Shannon S.
, p. 6738 - 6744 (2018/06/19)
An electrocatalytic method has been developed to oxidize primary alcohols and aldehydes to the corresponding carboxylic acids using 4-acetamido-2,2,6,6-tetramethylpiperidin-1-oxyl (ACT) as a mediator. The method successfully converts benzylic, aliphatic, heterocyclic, and other heteroatom-containing substrates to the corresponding carboxylic acids in aqueous solution at room temperature. The mild conditions enable retention of stereochemistry adjacent to the site of oxidation, as demonstrated in a 40 g-scale synthesis of a precursor to levetiracetam, a medication used to treat epilepsy.
Tetrapropylammonium perruthenate catalyzed glycol cleavage to carboxylic (Di)acids
Schmidt, Andrea-Katharina C.,Stark, Christian B. W.
supporting information; experimental part, p. 5788 - 5791 (2011/12/05)
A new method to accomplish glycol cleavage to carboxylic (di)acids in one step using catalytic amounts of tetrapropylammonium perruthenate (TPAP) together with N-methylmorpholine N-Oxide (NMO) as the stoichiometric oxidant is presented. In addition to regenerating the active catalyst, the N-oxide stabilizes intermediary carbonyl hydrates and thereby shifts a crucial equilibrium. The mild oxidation protocol is applicable to a broad range of substrates providing the respective acids, diacids, or keto acids in high yields.
Degradation of 1-deoxy-d-erythro-hexo-2,3-diulose in the presence of lysine leads to formation of carboxylic acid amides
Smuda, Mareen,Voigt, Michael,Glomb, Marcus A.
experimental part, p. 6458 - 6464 (2011/08/09)
A novel species of amides formed from degradation of one of the most important key intermediates in Maillard hexose chemistry-1-deoxyhexo-2,3- diulose-was investigated. In 1-deoxyhexo-2,3-diulose/Nα-t-BOC- lysine reaction mixtures four amides, Nε-acetyl lysine, N ε-formyl lysine, Nε-lactoyl lysine and N ε-glycerinyl lysine, were identified and their structures verified by authentic reference standards. Amides and corresponding carboxylic acids (acetic acid, formic acid, lactic acid and glyceric acid) accumulated over time. Both Nε-lysine amides and carboxylic acids were thus determined as stable Maillard end products. Results of model incubations suggested the synthesis of amides to be mechanistically closely related to the formation of their corresponding carboxylic acids by β-dicarbonyl cleavage. Due to the different chemical properties of all the compounds monitored, various analytical strategies had to be carried out (LC-MS2, GC-MS, GC-FID, enzymatic determination).
Synthetic studies towards 4,10-diaza-1,7-dioxaspiro[5.5]undecanes: access to 3-aza-6,8-dioxabicyclo[3.2.1]octan-2-one and 2H-1,4-oxazin-3(4H)-one frameworks
Goubert, Marlène,Toupet, Lo?c,Sinibaldi, Marie-Eve,Canet, Isabelle
, p. 8255 - 8266 (2008/02/08)
Synthetic approaches towards 4,10-diaza-1,7-dioxaspiro[5.5]undecanes starting from 1,3-dichloroacetone and solketal derivatives are explored. The method relies on the preparation of a key bis-substituted dihydroxy-protected oxime, which would undergo a final acidic deprotection-spiroacetalization process. Although the desired diazaspiroketal framework could not be obtained, our conditions led to the unexpected 3-aza-6,8-dioxabicyclo[3.2.1]octan-2-one 18 or to the oxazinone 32 in good yields.
Solution-phase and solid-phase syntheses of enzyme inhibitor RK-682 and antibiotic agglomerins
Schobert, Rainer,Jagusch, Garsten
, p. 6129 - 6132 (2007/10/03)
The enzyme inhibitor RK-682 (5A)-(+)-1 was prepared in solution and on a solid support from (2R)-glycerates in five steps and ca. 40% overall yield. Key steps were a ring-closing tandem addition-Wittig alkenation reaction of the respective protected or im
Synthetic studies of the cyclic depsipeptides bearing the 3-amino-6-hydroxy-2-piperidone (Ahp) unit. Total synthesis of the proposed structure of micropeptin T-20
Yokokawa, Fumiaki,Inaizumi, Akiko,Shioiri, Takayuki
, p. 1459 - 1480 (2007/10/03)
The first total synthesis of a cyclic depsipeptide possessing the 3-amino-6-hydroxy-2-piperidone (Ahp) unit was successfully achieved in a convergent manner by the oxidative construction of the Ahp unit at the later stage of the synthesis. This synthetic work provides data indicating that the structure of the target Ahp-depsipeptide, micropeptin T-20, should be re-examined.
NOVEL TRIAZOLE COMPOUNDS AS ANTIBACTERIAL AGENTS AND THEIR PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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Page/Page column 72-73, (2010/02/13)
The present invention relates to novel triazole compounds of formula (I), where all symbols are as defined in the detailed description; their pharmaceutically acceptable salts their stereosiomers thereof, their prodrugs, their rotamers, their pharmaceutical compositions containing them. The present invention also relates to a process for the preparation of the above said novel compounds.
Synthesis and CB1 receptor activities of novel arachidonyl alcohol derivatives
Parkkari, Teija,Savinainen, Juha R.,Rauhala, Anu L.,Tolonen, Tiina L.,Nevalainen, Tapio,Laitinen, Jarmo T.,Gynther, Jukka,Jaervinen, Tomi
, p. 3231 - 3234 (2007/10/03)
Novel derivatives of arachidonyl alcohol were synthesized and evaluated for their CB1 receptor activity by [35S]GTPγS assay using rat cerebellar membranes.
