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《Journal of Guangdong College of Pharmacy》 2005-06
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Modified synthesis of loratadine

ZHENG Xue-wen~1,JIANG Tao~2 (1.College of Pharmacy,Wuhan University,Hubei 430072,China;Department of Pharmacology,Guangdong College of Pharmacy,Guangzhou 510006,China)  
A modified procedure for the synthesis of loratadine is described.The readily available starting material,2-cyno-3-methylpyridine,was undertaken amidation in sulfuric acid,alkylation with butyl lithium and m-chlorobenzyl chloride,elimination in phosphorous oxychloride,Wittig reaction,hydrolysis and cyclization to give loratadine in 23.8% overall yield.A large-scale synthesis of loratadine has been developed that has been proved to be reproducible with few synthetic steps.
【Key Words】: loratadine synthesis
【CateGory Index】: TQ463
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