Vilsmeier-Haack试剂对4-羟基-2,5,6-三氨基嘧啶中的氨基保护和相关的化合物

Protection of Amino Groups in 4-Hydroxy-2,5,6-triaminopyrimidine with Vilsmeier-Haack Reagents and Relative Compounds

以 Vilsmeier- Haack试剂作为脒基化试剂研究了用于嘧啶衍生物中氨基的保护反应 ,将 4-羟基 - 2 ,5 ,6-三氨基嘧啶 ( )置于 Vilsmeier- Haack试剂中 ,在较强烈的反应条件下 ,得到氨基被保护了的新化合物 4-氯 - 2 ,5 ,6-三 (二甲氨亚甲氨基 )嘧啶 ( )。化合物 经氨水处理后 ,保护基被部分地脱除 ,主要转变成 6-氨基 - 4-氯 - 2 ,5 -二 (二甲氨亚甲氨基 )嘧啶 ( ) ,研究中发现 在硅胶的作用下 ,在氯仿 /甲醇洗脱液中容易形成化合物 :6-氨基 - 4-氯 - 2 -二甲氨亚甲氨基 - 5 -甲酰氨基嘧啶。另外 。

By reaction of 4 hydroxy 2,5,6 triaminopyrimidine (Ⅰ) with Vilsmeier Haack reagents under stronger reaction conditions new compound of 4 chloro 2,5,6 tri (dimethylamino methyleneamino) pyrimidine (Ⅱ) has been synthesised. Treatment of compound Ⅱ with aqueous ammonia mainly leads to produce 6 amino 4 chloro 2,5 di (dimethylaminomethyleneamino) pyrimidine (Ⅲ). It has been found that Ⅲ could easily be converted under the effect of silica gel into 6 amino 4 chloro 2 dimethylaminomethyleneamino 5 formamido pyrimidine (Ⅳ) in CHCl 3/MeOH. The physical properties of these new compounds have been also discussed.