81316-36-1Relevant academic research and scientific papers
Method for preparing spiro beta-lactam
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Paragraph 0048-0051, (2020/07/12)
The invention discloses a method for preparing spiro beta-lactam. The method comprises the following step: carrying out [2+1] cyclization reaction on beta-lactam and keto ester under the condition ofa phosphine catalyst to generate spiro beta-lactam. The
Carbene-Catalyzed Enantioselective Aromatic N-Nucleophilic Addition of Heteroarenes to Ketones
Liu, Yonggui,Luo, Guoyong,Yang, Xing,Jiang, Shichun,Xue, Wei,Chi, Yonggui Robin,Jin, Zhichao
supporting information, p. 442 - 448 (2019/11/25)
The aromatic nitrogen atoms of heteroarylaldehydes are activated by carbene catalysts to react with ketone electrophiles. Multi-functionalized cyclic N,O-acetal products are afforded in good to excellent yields and optical purities. Our reaction involves the formation of an unprecedented aza-fulvene-type acylazolium intermediate. A broad range of N-heteroaromatic aldehydes and electron-deficient ketone substrates works effectively in this transformation. Several of the chiral N,O-acetal products afforded through this protocol exhibit excellent antibacterial activities against Ralstonia solanacearum (Rs) and are valuable in the development of novel agrichemicals for plant protection.
High-Potency Phenylquinoxalinone Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Activators
Son, Jung-Ho,Zhu, Jie S.,Phuan, Puay-Wah,Cil, Onur,Teuthorn, Andrew P.,Ku, Colton K.,Lee, Sujin,Verkman, Alan S.,Kurth, Mark J.
, p. 2401 - 2410 (2017/04/03)
We previously identified phenylquinoxalinone CFTRact-J027 (4) as a cystic fibrosis transmembrane conductance regulator (CFTR) activator with an EC50 of ~200 nM and demonstrated its therapeutic efficacy in mouse models of constipation. Here, structure-activity studies were done on 36 synthesized phenylquinoxalinone analogs to identify compounds with improved potency and altered metabolic stability. Synthesis of the phenylquinoxalinone core was generally accomplished by condensation of 1,2-phenylenediamines with substituted phenyloxoacetates. Structure-activity studies established, among other features, the privileged nature of a properly positioned nitro moiety on the 3-aryl group. Synthesized analogs showed improved CFTR activation potency compared to 4 with EC50 down to 21 nM and with greater metabolic stability. CFTR activators have potential therapeutic indications in constipation, dry eye, cholestatic liver diseases, and inflammatory lung disorders.
GLUCOSYLCERAMIDE SYNTHASE INHIBITORS FOR THE TREATMENT OF DISEASES
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, (2015/04/15)
Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or conditions associated with the enzyme glucosylceramide synthase (GCS).
Facile synthesis of aryl α-keto esters via the reaction of aryl diazoacetate with H2O and DEAD
Guo, Zhenqiu,Huang, Haoxi,Fu, Qingquan,Hu, Wenhao
, p. 2486 - 2488 (2008/02/11)
A facile synthesis of aryl aα-keto esters in high yields is reported involving the reaction of aryl diazoacetate with H2O and diethyl azodicarboxylate (DEAD) catalyzed by dirhodium acetate. Georg Thieme Verlag Stuttgart.
Chiral β-diketonate ligands of 'pseudo planar chiral' topology: Enantioselective synthesis and transition metal complexation
Bocknack, Brian M.,Wang, Long-Cheng,Hughes, Freddie W.,Krische, Michael J.
, p. 6266 - 6275 (2007/10/03)
A practical enantioselective synthesis of chiral β-diketonate ligands 1a-1d, which are of 'pseudo planar-chiral' topology, is described. Additionally, the first chiral bis(diketonates) 2a-2c, ligands of C2-symmetry that are isoelectronic with r
BIARYL SUBSTITUTED PYRAZINONES AS SODIUM CHANNEL BLOCKERS
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Page/Page column 28-29, (2010/02/14)
Biaryl substituted pyrazinone compounds represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other thera
