Concise Synthesis of a Selective α1-Adrenoceptor Antagonist

…, M Matchett, P McGarry, S Sukhtankar…

文献索引：Connolly, Terrence J.; Matchett, Michael; McGarry, Patrick; Sukhtankar, Sunil; Zhu, Jiang Organic Process Research and Development, 2006 , vol. 10, # 3 p. 391 - 397

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被引用次数: 5

摘要

An efficient synthesis of an adrenoceptor antagonist has been developed and demonstrated in a pilot plant. A linear synthesis that relied on a catalytic reduction of a rather insoluble nitroaromatic proved to be a viable route. The active pharmaceutical ingredient (API) that contained an amidine functional group was generated from the amino-containing precursor by activation of dimethylacetamide (DMA) with phosphorus oxychloride (POCl3). The ...