- Design, synthesis, and biological activities of novel 2-alkylpyrrole derivatives
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To investigate the alkyl analog of insecticide chlorfenapyr, two series of 2-alkyl-4-bromo-5-(trifluoromethyl)pyrrole-3-carbonitriles were synthesized with a cycloaddition as the key step. The target products were characterized by 1H-NMR spectroscopy, elemental analysis, or HRMS. The insecticidal, herbicidal, and antifungal activities of the target compounds were evaluated and found that these compounds did not show much insecticidal activity, but compounds 4, 10, and 11 had very good fungicidal activities against Alternaria solani and Fusarium oxysporum. Moreover, compound 4 had an outstanding inhibition effect against pigweed.
- Li, Yongqiang,Wang, Ziwen,Zhang, Pengxiang,Liu, Yuxiu,Xiong, Lixia,Wang, Qingmin
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p. 1410 - 1414
(2015/04/27)
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- Organocatalytic synthesis of optically active β-branched α-amino esters via asymmetric biomimetic transamination
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This paper describes an efficient asymmetric biomimetic transamination of α-keto esters with a quinine-derived chiral base as the catalyst, giving a variety of β-branched α-amino esters in 50-96% yield and 87-95% ee. This journal is the Partner Organisations 2014.
- Su, Cunxiang,Xie, Ying,Pan, Hongjie,Liu, Mao,Tian, Hua,Shi, Yian
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p. 5856 - 5860
(2014/08/05)
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- Synthesis of α-amino acids by addition of putative azido radicals to α-methoxy acrylonitriles derived from aldehydes and ketones
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α-Methoxy acrylonitriles, available from aldehydes and ketones, react with sodium azide in the presence of ceric ammonium nitrate to give azido nitrates; from these compounds, α-amino acids are obtained by sequential treatment with sodium acetate in acetic acid and then methanolic potassium carbonate, followed by hydrogenation.
- Clive, Derrick L. J.,Etkin, Nola
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p. 2459 - 2462
(2007/10/02)
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- Highly selective tripeptide thrombin inhibitors
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Tripeptide aldehydes such as Boc-D-Phe-Pro-Arg-H (5l) exhibit potent direct inhibition of thrombin. This distinction offers important insight for the design of more potent and selective serine protease inhibitors which may be useful pharmacological tools and hold promise for development of clinically useful agents. The structure-activity relationships (SAR) on a series of anticoagulant peptides with high selectivity for the enzyme thrombin are discussed. The SAR is centered on a series of di- and tripeptide arginine aldehydes based on the structure of 5l. The structural and conformational role of the amino acid residue in position 1 was investigated by substitution with conformationally restricted aromatic amino acids, aromatic acids, and a dipeptide isostere containing the ψ[CH2N] amide bond replacement. Many of these peptides demonstrate potent antithrombotic activity along with selectivity toward thrombin, determined by comparison of in vitro inhibitory effects on trypsin, plasmin, factor Xa, and tissue plasminogen activator. Compound 5f, D-1-Tiq-Pro-Arg-H · sulfate is highly active and the most selective tripeptide aldehyde inhibitor of thrombin reported to date.
- Shuman,Rothenberger,Campbell,Smith,Gifford-Moore,Gesellchen
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p. 314 - 319
(2007/10/02)
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- The Synthesis of Amino Acids via Organoboranes
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The reaction of the acetate (1) with organoboranes provides a convenient, new route to amino acids.
- O'Donnell, Martin J.,Falmagne, Jean-Bernard
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p. 1168 - 1169
(2007/10/02)
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- STEREOISOMERIC CHIRAL 2,9-DIAZABICYCLODECANE-3,10-DIONES AS MODELS OF DIPEPTIDE GROUPING: SYNTHESIS, X-RAY, IR, NMR AND CD STUDIES
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Synthesis of the title optically active bicyclic dilactams I and II with cis- and trans-annelation of rings is described.The stereospecific synthesis started from (2R)-2-benzamido-2-(4-oxocyclohexyl)acetic acid ((-)-VI) whose absolute configuration was de
- Blaha, Karel,Farag, Ahmed M.,Helm, Dick van der,Hossain, Bilayet M.,Budesinsky, Milos,et al.
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p. 712 - 742
(2007/10/02)
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