Syntheses of apogalanthamine analogs as .ALPHA.-adrenergic blocking agents.
作者:SHIGERU KOBAYASHI、MASARU KIHARA、SATORU SHIZU、SADAMU KATAYAMA、HARUYOSHI IKEDA、KAZUO KITAHIRO、HIROSHI MATSUMOTO
DOI:10.1248/cpb.25.3312
日期:——
The apogalanthamine analogs, 10, 11-methylenedioxy-, 10, 11-dimethoxy-, and 11, 12-dimethoxy-5, 6, 7, 8-tetrahydrodibenz [c, e] azocines (2, 5, and 7, respectively) and their N-substituted derivatives (1, 3, 4, 6, 8, and 9) as α-adrenergic blocking agents, and the related compounds, 2, 3-dimethoxy-, 2, 3-methylenedioxy-, and 11-methoxy-5, 6, 7, 8-tetrahydrodibenz [c, e] azocines (10, 11, and 12, respectively) were synthesized by intramolecular cyclization of the corresponding amino-alcohols (30a-f) via the corresponding bromo-amines (16a-f). The preparation of the nitrovinyl compounds (19a-f) as startnig materials for the amino-alcohols was investigated. The conformation of these azocines was discussed in relation to nuclear magnetic resonance spectral data.
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