- Synthesis of Novel Pyrazine-Substituted 1 H -Pyrrole-2-carboxamides and Related Tethered Heterocycles
-
As part of a drug discovery program, 4-pyrazin-2-yl-1H-pyrrole-2-carboxamides were accessed along with a number of bicyclic analogues. Routes to these compounds were largely absent from the scientific literature. The synthesis of a 4-(pyrazin-2-yl)-1H-pyrrole-2-carboxamide and several fused bicyclic analogues all using standard procedures (SNAr, borylation, C C cross couplings, hydrolysis, amide bond formation, cyclisation, halogenation, and alkylation) from readily available starting materials is reported. The synthetic sequences range from 4-2 steps per final compound, with yields of isolated intermediates ranging from 20 to ?100%.
- Borrows, Rachel,Fairley, Gary,Feron, Lyman J. L.,Grant, Emma,Greenwood, Ryan D. R.,Howells, Rachel L.,Hughes, Samantha,Lamont, Scott G.,Lenz, Eva,McGuire, Thomas M.,Simpson, Iain
-
-
- 1,4-DISUBSTITUTED ISOQUINILONE DERIVATIVES AS RAF-KINASE INHIBITORS USEFUL FOR THE TREATMENT OF PROLIFERATIVE DISEASES
-
This invention relates to compounds of formula (I) wherein the variable substituents are described herein. The compounds are useful for the treatment of conditions and diseases characterized by an aberrant MAP kinase signaling pathway, such as cancer.
- -
-
Page/Page column 66
(2010/02/11)
-