63273-06-3Relevant articles and documents
Plladium-catalyzed arylation and heteroarylation of indolizines
Park, Choul-Hong,Ryabova, Victoria,Seregin, Ilya V.,Sromek, Anna W.,Gevorgyan, Vladimir
, p. 1159 - 1162 (2004)
A highly effective protocol for palladium-catalyzed selective arylation and heteroarylation of indolizines at C-3 has been developed. Mechanistic studies unambiguously support an electrophilic substitution pathway for this transformation.
Discovery of novel pyrrolopyridazine scaffolds as transient receptor potential vanilloid (TRPV1) antagonists
Dorange, Ismet,Forsblom, Rickard,MacSari, Istvan,Svensson, Mats,Besidski, Yevgeni,Blid, Jan,Sohn, Daniel,Gravenfors, Ylva,Bylund, Johan
, p. 6888 - 6895,8 (2020/09/02)
A novel indolizine class of compounds was identified as TRPV1 antagonist from an HTS campaign. However, this indolizine class proved to be unstable and reacted readily with glutathione when exposed to light and oxygen. Reactivity was reduced by the introduction of a nitrogen atom alpha to the indolizine nitrogen. The pyrrolopyridazine core obtained proved to be inert to the action of light and oxygen. The synthesis route followed the one used for the indolizine compounds, and the potency and ADMET profile proved to be similar.