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一步法合成硝唑尼特 被引量：2

Synthesis of Nitazoxanide by an One-step Process
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摘要 以乙酰水杨酸和2-氨基-5-硝基噻唑为原料,选用P2O5为脱水剂,经酰胺化反应一步合成了硝唑尼特〔2-乙酸基-N-(5-硝基-2-噻唑基)苯甲酰胺〕。研究了乙酰水杨酸、2-氨基-5-硝基噻唑、P2O5的用量,反应温度,酰胺化反应时间对收率的影响。较佳的合成工艺条件为:n(乙酰水杨酸)∶n(2-氨基-5-硝基噻唑)∶n(P2O5)=1.2∶1.0∶2.5,以DMF为溶剂,在90℃反应2.0 h,收率可达75%以上。 A new type of drug-nitazoxanide（2-acetyloxy-N-（5-nitro-2-thiazolyl）benzamide） was synthesized through amidation from acetylsalicylic acid and 2-amino-5-nitrothiazole at the presence of P2O5 as dehydrant.The effects of the amount of acetylsalicylic acid,2-amino-5-nitrothiazole and P2O5,the temperature and time of amidation on the yield were investigated.The optimal conditions were as follows：n（acetylsalicylic acid）∶n（2-amino-5-nitrothiazole）∶n（P2O5）=1.2∶1.0∶2.5,in DMF at 90 ℃ for 2.0 h.The yield can be higher than 75%.
作者 赵地顺 吕斌 段二红 张娟 寇成
机构地区 河北科技大学化学与制药工程学院 可北科技大学理学院 河北科技大学环境工程与科学学院
出处 《精细化工》 EI CAS CSCD 北大核心 2010年第12期1201-1203,共3页 Fine Chemicals
关键词 乙酰水杨酸 P2O5 一步合成 2-乙酸基-N-(5-硝基-2-噻唑基)苯甲酰胺 医药原料 acetylsalicylic acid P2O5 one-step synthesis 2-acetyloxy-N-（5-nitro-2-thiazolyl）benzamide drug materials
分类号 TQ460.6 [化学工程—制药化工] O626.1 [理学—有机化学]
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参考文献11

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二级参考文献16

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精细化工
2010年 第12期

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