| Title |
Synthesis of pyridyl substituted pyrazolo[4,3-c]pyridines as potential inhibitors of protein kinases |
| Authors |
Vilkauskaitė, Gytė ; Schaaf, Patricia ; Šačkus, Algirdas ; Krystof, Vladimir ; Holzer, Wolfgang |
| DOI |
10.3998/ark.5550190.p008.188 |
| Full Text |
|
| Is Part of |
Arkivoc.. Gainesville, FL : ARKAT USA. 2014, vol. 2014, iss. 2, p. 135-149.. ISSN 1551-7004. eISSN 1551-7012 |
| Keywords [eng] |
pyrazolones ; Sonogashira reaction ; multi-component reactions ; fused pyrazoles ; pyridines ; cyclin-dependent kinase (CDK) inhibitors ; 15N NMR spectroscopy |
| Abstract [eng] |
A synthetic route towards 3-(2-pyridyl)-6-(hetero)aryl-1H-pyrazolo[4,3-c]pyridines is described. The key step consists of a microwave-assisted multi-component reaction, including a Sonogashira type cross-coupling of appropriate 5-chloropyrazole-4-carbaldehydes with alkynyl- (hetero)arenes followed by pyridine ring formation of the coupling products in the presence of tert-butylamine, directly affording the title compounds. A congener without substituent at N-1 was accessed via cleavage of a tert-butyl protecting group. Detailed NMR spectroscopic studies (1H, 13C and 15N) were undertaken with the obtained compounds. Selected representatives were evaluated for their potential as inhibitors of protein kinases. |
| Published |
Gainesville, FL : ARKAT USA |
| Type |
Journal article |
| Language |
English |
| Publication date |
2014 |
| CC license |
|
