Indazoles: Regioselective protection and subsequent amine coupling reactions
(Chemical Equation Presented) Indazoles are unselectively protected under strongly basic conditions to give a mixture at N-1 and N-2. Under mildly acidic conditions, regioselective protection at N-2 takes place. Thermodynamic conditions lead to regioselective protection at N-1. This trend applies to various substituted indazoles. Protected 5-bromoindazoles participate in Buchwald reactions with a range of amines to generate novel derivatives.
Slade, David J.,Pelz, Nicholas F.,Bodnar, Wanda,Lampe, John W.,Watson, Paul S.
supporting information; experimental part
p. 6331 - 6334
(2009/12/26)
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