2357-39-3Relevant academic research and scientific papers
METALLOENZYME INHIBITOR COMPOUNDS
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Paragraph 0647; 0648; 0649; 0650, (2018/07/29)
Provided are compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
Synthesis-guided structure revision of the sarcodonin, sarcoviolin, and hydnellin natural product family
Lin, David W.,Masuda, Takeshi,Biskup, Moritz B.,Nelson, Jonathan D.,Baran, Phil S.
supporting information; experimental part, p. 1013 - 1030 (2011/04/15)
A sweeping structural revision of the sarcodonin natural product family (published structures 1a-13a) is proposed after extensive studies aimed at their chemical synthesis. Key features of revised structure 1b include replacement of the N,N-dioxide moiety with an oxime, ring-opening of the central diketopiperazine, and transposition of the terphenyl wing from the 1β-2β position of 1a to the 2β-3β position of 1b. This structure revision arose from the serendipitous synthesis of a benzodioxane aminal (44) whose structure was unambiguously determined by X-ray crystallography and whose spectral properties bore considerable resemblance to the published data for the sarcodonins. A versatile new method for O-arylation of hydroxamic acids is also reported herein, as well as a manganese(III)- mediated α-oxidation of hydroxamic acids to aminals.
SUBSTITUTED NITROGEN-CONTAINING SIX-MEMBERED AMINO-HETEROCYCLES AS VANILLOID-1 RECEPTOR ANTAGONISTS FOR TREATING PAIN
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Page/Page column 47-48, (2010/02/11)
The present invention provides a compound of formula (I): Y-J-NH-Z wherein: Y is a quinoline or isoquinoline optionally substituted with one or two substituents independently chosen from hydroxy, halogen, haloC1-4alkyl, C1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, nitro and amino; J is pyridine, pyridazine, pyrazine, pyrimidine or triazine optionally substituted with one or two substituents independently chosen from hydroxy, halogen, haloC1-4alkyl, C1-4alkyl, C3-5cycloalkyl, C1-4alkoxy, hydroxyC1-4alkyl, cyano, hydroxy, C1-4cycloalkoxy, C1-4alkylthio, haloC1-4alkoxy, nitro, Q, (CH2)pQ, NR2R3, -(CH2)pNR2R3 and -O(CH2)pNR2R3; wherein J is substituted at positions meta to each other by NH and Y; and Z is phenyl or pyridyl optionally substituted with one or two substituents independently selected from halogen, haloC1-4alkyl, C1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, nitro and amino; Q is phenyl, a five-membered heterocyclic ring containing one, two, three or four heteroatoms chosen from O, N and S, at most one heteroatom being O or S, or a six-membered heterocyclic ring containing one, two or three nitrogen atoms, optionally substituted by C1-4alkyl; each R2 and R3 is chosen from H and C1-4alkyl, or R2 and R3, together with the nitrogen atom to which they are attached, may form a six-membered ring optionally containing an oxygen atom or a further nitrogen atom, which ring is optionally substituted by C1-4alkyl or Q; p is 1, 2 or 3; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising it; its use in methods of therapy; use of it for manufacturing medicaments; and methods of using it to treat diseases requiring administration of a VR1 antagonist such as pain, cough, GERD and depression.
Eine neue Aminoazirin-Reaktion. Bildung von 3,6-Dihydropyrazin-2(1H)-onen
Hugener, Martin,Heimgartner, Heinz
, p. 172 - 179 (2007/10/02)
The reaction of 3-(dimethylamino)-2H-azirines 1 and 2-(trifluoromethyl)-1,3-oxazol-5(2H)-ones 5 in MeCN or THF at 50-80 deg leads to 5-(dimethylamino)-3,6-dihydropyrazin-2(1H)-ones 6 (Scheme 3).Reaction mechanisms for the formation of 6 are discussed: eit
UMWANDLUNG VON α-AMINOSAEUREN IN α-DIKETONE UEBER OXAZOLINZWISCHENSTUFEN
Leyendecker, Joachim,Niewoehner, Ulrich,Steglich, Wolfgang
, p. 2375 - 2378 (2007/10/02)
A four step sequence for the conversion of α-amino acids into α-diketones under mild conditions is desribed.
Gas chromatographic and mass spectrometric characteristics of 2-trifluoromethyl-3-oxazol-5-ones. A potentially useful derivative for α-amino acids
Ferrito,Borg,Eagles,Fenwick
, p. 499 - 501 (2007/10/08)
The mass spectra of a number of 2-trifluoromethyl-3-oxazol-5-ones, prepared from protein amino acids, have been recorded. The compounds have been separated by gas chromatography using binary column techniques. Analysis of the mass spectra has identified m
