Superacid cyclodehydration of ketones in the production of tricyclic antihistamines

…, BL Murphy, JE Clark, P Tahbaz, TA Mann

文献索引：Schumacher, Doris P.; Murphy, Bruce L.; Clark, Jon E.; Tahbaz, Pete; Mann, Thomas A. Journal of Organic Chemistry, 1989 , vol. 54, # 9 p. 2242 - 2244

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被引用次数: 29

摘要

Loratadine (Sch 29851; 1) is a potent, long-acting antihistamine with a lack of central nervous system (CNS) side effects.'Although the compound is a derivative of azatadine (2), the presence of a chlorine in the phenyl ring causes unique problems such that the azatadine process, which requires two reduction steps, cannot be effectively used, as the chlorine is in part removed. 2 In addition, formation of the tricyclic ring structure with ...