343781-41-9Relevant articles and documents
PYRAZOLE AMIDE DERIVATIVE
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Page/Page column 152, (2015/09/28)
The present invention relates to a novel compound having a function of inhibiting RORγ activity. The present invention also relates to pharmaceutical composition comprising the compound, a use of the compound in treating or preventing autoimmune diseases, inflammatory diseases, metabolic diseases, or cancer diseases.
Deprotonation of chloropyridines using lithium magnesates
Awad, Ha?an,Mongin, Florence,Trécourt, Fran?ois,Quéguiner, Guy,Marsais, Francis
, p. 7873 - 7877 (2007/10/03)
Chloropyridines are deprotonated using lithium magnesates. 4-Chloropyridine was deprotonated on treatment with 1/3 equiv of the highly coordinated magnesate Bu3(TMP)MgLi2 in THF at -10°C, as evidenced by trapping with I2. The use of Bu(TMP)2MgLi in Et 2O allowed the reaction of 2-chloropyridine, giving the 3-functionalized derivative as the main product. Mixtures of 3- and 4-functionalized derivatives were obtained when 2,6-dichloropyridine was involved in the reaction. Performing the reaction on 3-chloropyridine with lithium magnesates in THF, either the 4,4′-dimer or the 4-iodo derivative was formed after quenching by I2, the former using 1/3 equiv of Bu2(TMP)MgLi and the latter using 1 equiv of (TMP)3MgLi. Similar results were observed with 3,5-dichloropyridine, 2,5-dichloropyridine and 3-chloro-2-fluoropyridine. 1,2-Migration of the lithium arylmagnesate formed by deprotonation was proposed to justify the dimers formation.