Method for preparing multi-substituted quinazoline and heterocyclic pyrimidine derivative

2012 
The invention discloses a method for preparing a multi-substituted quinazoline and heterocyclic pyrimidine derivative. The method comprises the following step of: performing cyclization reaction on substituted o-halogenated aromatic aldehyde/ ketone shown as a formula II and alcohol shown as a formula III in the presence of aqueous ammonia, oxidant and catalyst to obtain a compound shown as a formula I, wherein the catalyst is a copper salt, and the substituted o-halogenated aromatic aldehyde/ ketone shown as the formula II is single-substituted or multi-substituted o-halogenated aromatic aldehyde/ ketone. The method for synthesizing the multi-substituted quinazoline and heterocyclic pyrimidine derivative shown as the formula I is a one-step synthesizing method, and the method has the following characteristics that (1) the catalyst is cheap and readily available, the reaction operation is simple, and the method is suitable for large-scale production; (2) the catalyst system has extremely high chemical reaction property and selectivity, and the multi-substituted quinazoline and heterocyclic pyrimidine derivative can be synthesized with high yield; and (3) the catalyst system has strong universality to substrates, and the substrates containing various functional groups can efficiently react.
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