Novel synthesis of 2-butyl-5-chloro-3H-imidazole-4-carbaldehyde: A key intermediate of Losartan

Hai Bo Sun Guo Jun Zheng Ya Ping Wang Xiang Jing Wang Wen Sheng Xiang

引用本文: Hai Bo Sun,  Guo Jun Zheng,  Ya Ping Wang,  Xiang Jing Wang,  Wen Sheng Xiang. Novel synthesis of 2-butyl-5-chloro-3H-imidazole-4-carbaldehyde: A key intermediate of Losartan[J]. Chinese Chemical Letters, 2009, 20(3): 269-270. doi: 10.1016/j.cclet.2008.11.031 shu
Citation:  Hai Bo Sun,  Guo Jun Zheng,  Ya Ping Wang,  Xiang Jing Wang,  Wen Sheng Xiang. Novel synthesis of 2-butyl-5-chloro-3H-imidazole-4-carbaldehyde: A key intermediate of Losartan[J]. Chinese Chemical Letters, 2009, 20(3): 269-270. doi: 10.1016/j.cclet.2008.11.031 shu

Novel synthesis of 2-butyl-5-chloro-3H-imidazole-4-carbaldehyde: A key intermediate of Losartan

  • 基金项目:

    This study was financially supported by Outstanding Youth Foundation of Heilongjiang Province (No. JC200706).

摘要: Anovelmethod for synthesis of 2-butyl-5-chloro-3H-imidazole-4-carbaldehyde 2, a key intermediate of Losartan was reported. The compound 2 was synthesized fromstarting material dimethyl malonate 6 and n-valeronitrile 8 by six steps with an overall yield of 40%.The key step including the reaction of compound 5 with POCl3/DMF followed by hydrolysis to give compound 2 with the yield of 68%.

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  • 收稿日期:  2008-07-17
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