一步法合成硝唑尼特

Synthesis of Nitazoxanide by an One-step Process

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的用量和反应温度、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90℃反应2.0h，收率可达到75%以上。

Abstract:

A newtype drug-nitazoxanide (2-Acetyloxy-N-(5-nitro-2-thiazolyl)benzamide) was synthesized through amidation from acetylsalicylic acid and 2-Amino-5-nitrothiazole in 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 2.0h, the yield can be higher than 75%.