A regioselective approach to 5-substituted-3-amino-1,2,4-triazines

被引:20
作者
Limanto, J [1 ]
Desmond, RA [1 ]
Gauthier, DR [1 ]
Devine, PN [1 ]
Reamer, RA [1 ]
Volante, RP [1 ]
机构
[1] Merck & Co Inc, Merck Res Labs, Dept Proc Res, Rahway, NJ 07065 USA
关键词
D O I
10.1021/ol034602+
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Nucleophilic displacement of readily available alpha,alpha-dibromoketones with excess morpholine gave the corresponding ketoaminals, which upon condensation with aminoguanidine in MeOH in the presence of AcOH afforded 5-substituted-3-amino-1,2,4-triazines in >95% regioselectivity and 45-76% isolated yield.
引用
收藏
页码:2271 / 2274
页数:4
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