Process development of the synthetic route to sulamserod hydrochloride

BA Kowalczyk, James Robinson, III, and…

文献索引：Kowalczyk, Bruce A.; Robinson III, James; Gardner, John O. Organic Process Research and Development, 2001 , vol. 5, # 2 p. 116 - 121

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被引用次数: 4

摘要

Sulamserod hydrochloride is a potent 5-HT4 receptor antagonist and was a clinical candidate for the treatment of gastrointestinal disorders. Process development of the fairly long synthetic route (12 linear, 14 overall steps) was undertaken. Process improvements were highlighted by aromatic chlorination choices in making dichlorobenzodioxan 2 and acetylaminochloroketone 7, a transfer hydrogenation reducing a nitro group and ...