【摘要】 2-羟基-5,7-二甲基-1,2,4-三唑[1,5-a]嘧啶(TPO)是三唑并嘧啶类衍生物的重要中间体,以氨基脲盐酸盐为起始原料,经环化、硝化、还原及并环得到.氨基脲盐酸盐先与甲酸成环,制得中间1,2,4-三唑-5-酮(TO),产率86.5%;用发烟硝酸硝化得3-硝-基1,2,4-三唑-5-酮(NTO),产率90.1%;雷尼镍催化下加氢还原得3-氨基-5-羟基-1,2,4-三唑(ATO),产率88.0%;最后与乙酰丙酮环合制得标题化合物TPO,产率86.0%.该方法原料易得、操作简便,总收率较高,达到59.0%.更多还原

【Abstract】 The 2-hydroxyl-5,7-dimethyl-1,2,4-triazolopyrimidine（TPO） is an important intermediate for triazolopyrimidine derivatives.It was synthesized from amidourea hydrochloride by way of ring closure,nitration,deoxidization and cyclization.First,amidourea hydrochloride reacted with formyl acid to form 1,2,4-triazol-5-one（TO） with a yield of 86.5%.Second,the TO was nitrated using fuming nitric acid to prepare the 3-nitro-1,2,4-triazol-5-one（NTO） with a yield of 90.1%.Third,NTO was reduced by using H₂ in the presence of Raney Ni to obtain the 3-amino-5-hydroxyl-1,2,4-triazole（ATO） with a yield of 88.0%.The TPO was then synthesized from ATO together with acetyl acetone with a yield of 86.0%.The overall yield was 59.0%.The synthesis route used is simple.The reaction conditions are mild.And the raw materials are cheap and easy to obtain.更多还原