2-正丁基-4-氯-5-甲酰基咪唑合成新工艺

Novel Syntheses of 2-Butyl-5-chloro-1H-imidazole-4-carboxaldehyde

以戊腈为原料,经加成、取代得到脒(2),再与乙二醛缩合、脱一分子水得到咪唑啉酮化合物(3),最后经氯代、氧化后得到2-正丁基-4-氯-5-甲酰基咪唑,收率40.5%。该工艺具有原料易得,反应条件温和,合成路线短,易于工业化生产等特点,是一条新的2-正丁基-4-氯-5-甲酰基咪唑(1)合成路线。

2 - Butyl - 5 - chloro - 1 H - imidazole - 4 - carboxaldehyde was synthesized from valeronitrile by addition with CH3OH/HC1, substitution to afford pentanimidamide hydrochloride,which subsequently subjected to condensation with aqueous solution of glyoxal, dehydration to give 2 - butyl - 1H - imidazol -4（5H） -one, which was subjected to chlorination and then oxidation in yield of 40.5%. The route was new route to synthesis of 2 - butyl - 5 - chloro - 1H - imidazole - 4 - carboxaldehyde, which has some advantages such as availability of raw materials, mild reaction condition, short synthesized route, good yields, and suitable for industrial- scale production.