An optimized procedure for direct access to 1: H -indazole-3-carboxaldehyde derivatives by nitrosation of indoles
Indazole derivatives are currently drawing more and more attention in medicinal chemistry as kinase inhibitors. 1H-indazole-3-carboxaldehydes are key intermediates to access to a variety of polyfunctionalized 3-substituted indazoles. We report here a general access to this motif, based on the nitrosation of indoles in a slightly acidic environment. These very mild conditions allow the conversion of both electron-rich and electron-deficient indoles into 1H-indazole-3-carboxaldehydes.
3-Benzimidazol-2-yl-1H-indazoles as potent c-ABL inhibitors
The 3-benzimidazol-2-yl-1H-indazole scaffold was developed as an alternate scaffold for our receptor tyrosine kinase (RTK) inhibitor program. In exploring the SAR of this series, it was discovered that a subset of these compounds potently inhibit the enzy
McBride, Christopher M.,Renhowe, Paul A.,Gesner, Thomas G.,Jansen, Johanna M.,Lin, Julie,Ma, Sylvia,Zhou, Yasheen,Shafer, Cynthia M.
p. 3789 - 3792
(2008/12/23)
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