86944-08-3Relevant academic research and scientific papers
The effect of pKa on pyrimidine/pyridine-derived histamine H4 ligands
Savall, Brad M.,Meduna, Steven P.,Venable, Jennifer,Wei, Jianmei,Smith, Russell C.,Hack, Michael D.,Thurmond, Robin L.,McGovern, Patricia,Edwards, James P.
, p. 5489 - 5492 (2014)
During the course of our efforts toward the discovery of human histamine H4 antagonists from a series of 2-aminiopyrimidines, it was noted that a 6-trifluoromethyl group dramatically reduced affinity of the series toward the histamine H4 receptor. This observation was further investigated by synthesizing a series of ligands that varied in pKa of the pyrimidine derived H4 ligands by over five orders of magnitude and the effect on histamine H4 affinity. This trend was then extended to the discovery of C-linked piperidinyl-2-amino pyridines as histamine H4 receptor antagonists.
CYCLOPHILIC REATIONS OF ALLENE-1,3-DICARBOXYLIC ESTER. PART 7. SYNTHESIS OF BICYCLIC AND TRICYCLIC HETEROCYCLIC COMPOUNDS INVOLVING NITROGEN, SULPHUR, AND CARBON AS NUCLEOPHILES
Doad, Gurinder J. S.,Okor, Dorcas I.,Scheinmann, Feodor,Bates, Paul A.,Hursthouse, Michael B.
, p. 2993 - 3004 (2007/10/02)
Dimethyl allene-1,3-dicarboxylate (1) is an excellent substrate for heterocyclic syntheses giving products with esters side-chains capable of further elaboration. The allene (1) has been converted into the condensed pyridones (8)-(13) by reactions with 2-
