34589-97-4Relevant academic research and scientific papers
The reaction of prop-2-ynylsulfonium salts and sulfonyl-protected β-amino ketones to epoxide-fused 2-methylenepyrrolidines and S-containing pyrroles
Jia, Tingting,Zeng, Gongruixue,Zhang, Chong,Zeng, Linghui,Zheng, Wenya,Li, Siyao,Wu, Keyi,Shao, Jiaan,Zhang, Jiankang,Zhu, Huajian
supporting information, p. 2657 - 2660 (2021/03/16)
A novel divergent domino annulation reaction of prop-2-ynylsulfonium salts with sulfonyl-protected β-amino ketones has been developed, affording various epoxide-fused 2-methylenepyrrolidines and S-containing pyrroles in moderate to excellent yields. Prop-2-ynylsulfonium salts act as C2synthons in the reactions providing a promising epoxide-fused skeleton in a single operation with readily accessible starting materials.
Synthesis of 2-Amino Substituted Oxazoles from α-Amino Ketones and Isothiocyanates via Sequential Addition and I2-Mediated Desulfurative Cyclization
Chang, Junbiao,Yu, Wenquan,Zhang, Shuangshuang,Zhao, Qiongli,Zhao, Yifei
supporting information, (2020/04/29)
Oxazol-2-amines were synthesized by annulation of α-amino ketones and isothiocyanates. This sequential synthetic process involves addition of α-amino ketones to isothiocyanates and I2-promoted desulfurative cyclization omitting isolation of the less stable thiourea intermediates. It is transition metal-free and operationally simple, providing access to a variety of 2-amino substituted oxazole derivatives under mild reaction conditions. (Figure presented.).
Synthetic method for 2,5-diaryloxazole compounds and anti-inflammatory pharmaceutical compounds containing the 2,5-diaryloxazole compounds
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Paragraph 0060; 0070-0073, (2019/02/02)
The present inventors have invented an effective synthesis method for a 2,5-diaryloxazole compound from a commercially available starting material. The synthesis method uses the Delepine reaction and the Robinson-Gabriel reaction as main steps. For oxazole compounds synthesized in the present invention, the present inventors have evaluated the inhibitory effect of LPS-induced NO production in RAW 264.7 cells, and have found that the oxazole compounds of the present invention significantly inhibit NO production in a concentration-dependent manner. Therefore, the oxazole compounds of the present invention may be potential compounds which can be used as anti-inflammatory agents.COPYRIGHT KIPO 2018
Anti-inflammatory pharmaceutical compounds containing 2,5-diaryloxazole compounds
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Paragraph 0023; 0033; 0034; 0036, (2019/02/21)
The present invention efficiently diaryloxazole compounds inside the victims of the commercial starting material from 2, 5 - configurated. The synthesis [...] (Delepine) [pu [pu] l - the adventures reaction a hole of major steps reaction. In the present invention synthesized oxazole compounds the present invention with respect to the victims of the RAW 264. 7 NO generation have caused LPS - in assessing, oxazole compounds of the present invention depending on the concentration of the present invention were found to significantly NO billion number generation number may be likely oxazole compounds are anti-inflammatory compound as a lever with each other. (by machine translation)
Efficient Synthesis and In Vitro Biological Evaluation of 2,5-Diaryloxazoles as Potential Nitric Oxide Production Inhibitors
Jang, Ha Young,Damodar, Kongara,Kim, Jin-Kyung,Jun, Jong-Gab
, p. 1481 - 1485 (2017/12/04)
An efficient first synthesis of 2,5-diaryloxazoles 1–5 was accomplished from commercially inexpensive precursors and in overall yields of 38–48%. The synthesis proceeds via α-aminoketones and cyclodehydration (Robinson–Gabriel reaction) as key step. Next, these oxazoles were examined for their inhibitory effect against nitric oxide (NO) production in lipopolysaccharide (LPS)-induced RAW 264.7 cells and were found to display concentration-dependent inhibition of NO production without cytotoxicity. Of note, compound 3 (70.7%; IC50 = 2.33 μM) was identified as a potent inhibitor in view of its comparable inhibitory effect with the positive control, NG-monomethyl-L-arginine acetate (L-NMMA) (79.3%; IC50 = 4.51 μM) followed by compounds 5 (68.3%; IC50 = 2.30 μM) and 2 (53.9%; IC50 = 6.31 μM). As a whole, compound 3 may hold great promise for further development of NO production targeted anti-inflammatory agent.
4-ARYLPYRROLE SUBSTITUTED 2-INDOLINE DERIVATIVES ACTIVE AS PROTEIN KINASE INHIBITORS
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, (2009/01/20)
The present invention relates to certain 4-arylpyrrole substituted 2-indolinone compounds of Formula (I), which modulate the activity of protein kinases (PKs). The compounds of this invention are therefore useful in treating disorders related to dysregula
COMPOUNDS, METHODS AND FORMULATIONS FOR THE ORAL DELIVERY OF A GLUCAGON LIKE PEPTIDE (GLP)-1 COMPOUND OR AN MELANOCORTIN 4 RECEPTOR (MC4) AGONIST PEPTIDE
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Page/Page column 42, (2008/06/13)
The present invention relates to novel compounds, methods, and formulations useful for the oral delivery of a GLP-1 compound or an MC4 agonist peptide.
ANTIBACTERIAL BENZOIC ACID DERIVATIVES
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Page 358, (2010/02/06)
The invention provides antimicrobial agents and methods of using the agents for sterilization, sanitation, antisepsis, disinfection, and treatment of infections in mammals.
